Opioid receptors in GtoPdb v.2023.1 Opioid receptors in GtoPdb v.2023.1

Opioid and opioid-like receptors are activated by a variety of endogenous peptides including [Met]enkephalin (met), [Leu]enkephalin (leu), βendorphin (β-end), α-neodynorphin, dynorphin A (dynA), dynorphin B (dynB), big dynorphin (Big dyn), nociceptin/orphanin FQ (N/OFQ); endomorphin-1 and endomorphin-2 are also potential endogenous peptides. The Greek letter nomenclature for the opioid receptors, μ, δ and κ, is well established, and NC-IUPHAR considers this nomenclature appropriate, along with the symbols spelled out (mu, delta, and kappa), and the acronyms, MOP, DOP, and KOP [124, 101, 92]. However the acronyms MOR, DOR and KOR are still widely used in the literature. The human N/OFQ receptor, NOP, is considered 'opioid-related' rather than opioid because, while it exhibits a high degree of structural homology with the conventional opioid receptors [304], it displays a distinct pharmacology. Currently there are numerous clinically used drugs, such as morphine and many other opioid analgesics, as well as antagonists such as naloxone. The majority of clinically used opiates are relatively selective μ agonists or partial agonists, though there are some μ/κ compounds, such as butorphanol, in clinical use. κ opioid agonists, such as the alkaloid nalfurafine and the peripherally acting peptide difelikefalin, are in clinical use for itch.

[1]  B. Roth,et al.  Structures of the entire human opioid receptor family , 2023, Cell.

[2]  Samuel T. Slocum,et al.  Structure-based design of bitopic ligands for the µ-opioid receptor , 2022, Nature.

[3]  Xi Cheng,et al.  Molecular recognition of morphine and fentanyl by the human μ-opioid receptor , 2022, Cell.

[4]  Graeme Henderson,et al.  Biased Agonism: Lessons from Studies of Opioid Receptor Agonists. , 2022, Annual review of pharmacology and toxicology.

[5]  G. Skiniotis,et al.  Structure‐Based Evolution of G Protein‐Biased μ‐Opioid Receptor Agonists , 2022, bioRxiv.

[6]  Joseph M. Paggi,et al.  Insights into distinct signaling profiles of the µOR activated by diverse agonists , 2022, Nature Chemical Biology.

[7]  M. J. Robertson,et al.  Structure Determination of Inactive-State GPCRs with a Universal Nanobody , 2021, bioRxiv.

[8]  V. Sreenivasan,et al.  Intrinsic Efficacy of Opioid Ligands and Its Importance for Apparent Bias, Operational Analysis, and Therapeutic Window , 2020, Molecular Pharmacology.

[9]  Elyssa B. Margolis,et al.  Biased signaling by endogenous opioid peptides , 2020, Proceedings of the National Academy of Sciences.

[10]  N. Nic Daéid,et al.  Activation of μ‐opioid receptors by MT‐45 (1‐cyclohexyl‐4‐(1,2‐diphenylethyl)piperazine) and its fluorinated derivatives , 2020, British Journal of Pharmacology.

[11]  Reid H. J. Olsen,et al.  Nanobody-enabled monitoring of kappa opioid receptor states , 2020, Nature Communications.

[12]  C. Ruzza,et al.  Detailed In Vitro Pharmacological Characterization of the Clinically Viable Nociceptin/Orphanin FQ Peptide Receptor Antagonist BTRX-246040 , 2020, The Journal of Pharmacology and Experimental Therapeutics.

[13]  Peter Buneman,et al.  Why data citation isn't working, and what to do about it , 2020, Database J. Biol. Databases Curation.

[14]  J. Streicher,et al.  A Novel Mu-Delta Opioid Agonist Demonstrates Enhanced Efficacy with Reduced Tolerance and Dependence in Mouse Neuropathic Pain Models. , 2020, The journal of pain : official journal of the American Pain Society.

[15]  Andrew M. Piggott,et al.  A tetrapeptide class of biased analgesics from an Australian fungus targets the µ-opioid receptor , 2019, Proceedings of the National Academy of Sciences.

[16]  V. Tékus,et al.  A Novel G Protein–Biased Agonist at the δ Opioid Receptor with Analgesic Efficacy in Models of Chronic Pain , 2019, The Journal of Pharmacology and Experimental Therapeutics.

[17]  Xinzhong Dong,et al.  Discovery of Benzamidine- and 1-Aminoisoquinoline-Based Human MAS-Related G-Protein-Coupled Receptor X1 (MRGPRX1) Agonists. , 2019, Journal of medicinal chemistry.

[18]  Steven J Brown,et al.  Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140). , 2019, Journal of medicinal chemistry.

[19]  D. Selley,et al.  Design, Synthesis, and Biological Evaluation of the Third Generation 17-Cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan (NAP) Derivatives as μ/κ Opioid Receptor Dual Selective Ligands. , 2019, Journal of medicinal chemistry.

[20]  S. Salvadori,et al.  In vitro and in vivo characterization of the bifunctional μ and δ opioid receptor ligand UFP‐505 , 2018, British journal of pharmacology.

[21]  S. Novello,et al.  Anti‐Parkinsonian and anti‐dyskinetic profiles of two novel potent and selective nociceptin/orphanin FQ receptor agonists , 2018, British journal of pharmacology.

[22]  Kathryn E. Livingston,et al.  Pharmacologic Evidence for a Putative Conserved Allosteric Site on Opioid Receptors , 2018, Molecular Pharmacology.

[23]  Ryan T. Strachan,et al.  Structure of the Nanobody-Stabilized Active State of the Kappa Opioid Receptor , 2018, Cell.

[24]  W. Rubas,et al.  NKTR-181: A Novel Mu-Opioid Analgesic with Inherently Low Abuse Potential , 2017, The Journal of Pharmacology and Experimental Therapeutics.

[25]  Henry Lin,et al.  Structure-based discovery of opioid analgesics with reduced side effects , 2016, Nature.

[26]  M. von Zastrow,et al.  Molecular Pharmacology of δ-Opioid Receptors , 2016, Pharmacological Reviews.

[27]  R. Stevens,et al.  The Importance of Ligand-Receptor Conformational Pairs in Stabilization: Spotlight on the N/OFQ G Protein-Coupled Receptor. , 2015, Structure.

[28]  M. Bruchas,et al.  Quantitative Signaling and Structure-Activity Analyses Demonstrate Functional Selectivity at the Nociceptin/Orphanin FQ Opioid Receptor , 2015, Molecular Pharmacology.

[29]  P. Pinton,et al.  Pharmacological Profile of Nociceptin/Orphanin FQ Receptors Interacting with G-Proteins and β-Arrestins 2 , 2015, PloS one.

[30]  Stephen M. Husbands,et al.  Structural insights into μ-opioid receptor activation , 2015, Nature.

[31]  Kathryn E. Livingston,et al.  Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor. , 2015, Journal of medicinal chemistry.

[32]  N. Zaveri,et al.  Discovery of the First Small-Molecule Opioid Pan Antagonist with Nanomolar Affinity at Mu, Delta, Kappa, and Nociceptin Opioid Receptors , 2015, ACS chemical neuroscience.

[33]  Anton Barty,et al.  Structural basis for bifunctional peptide recognition at human δ-Opioid receptor , 2015, Nature Structural &Molecular Biology.

[34]  L. Devi,et al.  Challenges for opioid receptor nomenclature: IUPHAR Review 9 , 2015, British journal of pharmacology.

[35]  S. Salvadori,et al.  In vitro and in vivo pharmacological characterization of nociceptin/orphanin FQ tetrabranched derivatives , 2014, British journal of pharmacology.

[36]  E. Bullmore,et al.  The opioid receptor pharmacology of GSK1521498 compared to other ligands with differential effects on compulsive reward-related behaviours , 2014, Psychopharmacology.

[37]  K. Schiene,et al.  Cebranopadol: A Novel Potent Analgesic Nociceptin/Orphanin FQ Peptide and Opioid Receptor Agonist , 2014, The Journal of Pharmacology and Experimental Therapeutics.

[38]  D. McKinzie,et al.  Discovery of a novel series of orally active nociceptin/orphanin FQ (NOP) receptor antagonists based on a dihydrospiro(piperidine-4,7'-thieno[2,3-c]pyran) scaffold. , 2014, Journal of medicinal chemistry.

[39]  P. Veinante,et al.  A mu–delta opioid receptor brain atlas reveals neuronal co-occurrence in subcortical networks , 2014, Brain Structure and Function.

[40]  D. McKinzie,et al.  LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders , 2014, Neuropharmacology.

[41]  Bryan L. Roth,et al.  Molecular control of δ-opioid receptor signalling , 2014, Nature.

[42]  A. M. Phillips,et al.  Development of Functionally Selective, Small Molecule Agonists at Kappa Opioid Receptors* , 2013, The Journal of Biological Chemistry.

[43]  G. Pasternak,et al.  Mu Opioids and Their Receptors: Evolution of a Concept , 2013, Pharmacological Reviews.

[44]  Bryan L. Roth,et al.  Selective κ Opioid Antagonists nor-BNI, GNTI and JDTic Have Low Affinities for Non-Opioid Receptors and Transporters , 2013, PloS one.

[45]  M. Banks,et al.  Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor , 2013, Proceedings of the National Academy of Sciences.

[46]  B. Bradley,et al.  Amygdala-Dependent Fear Is Regulated by Oprl1 in Mice and Humans with PTSD , 2013, Science Translational Medicine.

[47]  M. Morari,et al.  Acute and chronic antiparkinsonian effects of the novel nociceptin/orphanin FQ receptor antagonist NiK‐21273 in comparison with SB‐612111 , 2013, British journal of pharmacology.

[48]  B. Kieffer,et al.  Impaired Hippocampus-Dependent and Facilitated Striatum-Dependent Behaviors in Mice Lacking the Delta Opioid Receptor , 2013, Neuropsychopharmacology.

[49]  M. Spetea,et al.  Discovery and biological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist , 2012, BMC Pharmacology and Toxicology.

[50]  P. Wade,et al.  Identification of a dual δ OR antagonist/μ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d). , 2012, Bioorganic & medicinal chemistry letters.

[51]  Aashish Manglik,et al.  Structure of the δ-opioid receptor bound to naltrindole , 2012, Nature.

[52]  J. Neumeyer,et al.  Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors. , 2012, Journal of medicinal chemistry.

[53]  Bryan L. Roth,et al.  Structure of the Nociceptin/Orphanin FQ Receptor in Complex with a Peptide Mimetic , 2012, Nature.

[54]  L. Pardo,et al.  Crystal structure of the μ-opioid receptor bound to a morphinan antagonist , 2012, Nature.

[55]  D. Lambert,et al.  Pharmacological characterization of the bifunctional opioid ligand H-Dmt-Tic-Gly-NH-Bzl (UFP-505). , 2012, British journal of anaesthesia.

[56]  B. Kieffer,et al.  Localization and regulation of fluorescently labeled delta opioid receptor, expressed in enteric neurons of mice. , 2011, Gastroenterology.

[57]  G. Pasternak,et al.  Generation of novel radiolabeled opiates through site-selective iodination. , 2011, Bioorganic & medicinal chemistry letters.

[58]  Timothy J Kropp,et al.  Uniform assessment and ranking of opioid μ receptor binding constants for selected opioid drugs. , 2011, Regulatory toxicology and pharmacology : RTP.

[59]  R. Maldonado,et al.  Deletion of the δ Opioid Receptor Gene Impairs Place Conditioning But Preserves Morphine Reinforcement , 2011, Biological Psychiatry.

[60]  S. Husbands,et al.  The First Universal Opioid Ligand, (2S)-2-[(5R,6R,7R,14S)-N-cyclopropylmethyl-4,5-epoxy-6,14-ethano-3-hydroxy-6-methoxymorphinan-7-yl]-3,3-dimethylpentan-2-ol (BU08028): Characterization of the In Vitro Profile and In Vivo Behavioral Effects in Mouse Models of Acute Pain and Cocaine-Induced Reward , 2011, Journal of Pharmacology and Experimental Therapeutics.

[61]  Walter A. Korfmacher,et al.  Pharmacological profile of the NOP agonist and cough suppressing agent SCH 486757 (8-[Bis(2-Chlorophenyl)Methyl]-3-(2-Pyrimidinyl)-8-Azabicyclo[3.2.1]Octan-3-Ol) in preclinical models. , 2010, European journal of pharmacology.

[62]  N. Zaveri,et al.  Comparison of the Antinociceptive and Antirewarding Profiles of Novel Bifunctional Nociceptin Receptor/μ-Opioid Receptor Ligands: Implications for Therapeutic Applications , 2009, Journal of Pharmacology and Experimental Therapeutics.

[63]  Adam J Kuszak,et al.  Purification and functional reconstitution of monomeric mu-opioid receptors: allosteric modulation of agonist binding by Gi2. , 2009, The Journal of biological chemistry.

[64]  T. Graczyk,et al.  Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747). , 2009, Journal of medicinal chemistry.

[65]  S. Salvadori,et al.  Pharmacological characterization of the nociceptin/orphanin FQ receptor non peptide antagonist Compound 24. , 2009, European journal of pharmacology.

[66]  J. Bidlack,et al.  Syntheses of novel high affinity ligands for opioid receptors. , 2009, Bioorganic & medicinal chemistry letters.

[67]  L. Terenius Stereospecific interaction between narcotic analgesics and a synaptic plasm a membrane fraction of rat cerebral cortex. , 2009, Acta pharmacologica et toxicologica.

[68]  J. Lötsch,et al.  A Common Human μ-Opioid Receptor Genetic Variant Diminishes the Receptor Signaling Efficacy in Brain Regions Processing the Sensory Information of Pain* , 2009, Journal of Biological Chemistry.

[69]  E. Kostenis,et al.  Pharmacological profile of NOP receptors coupled with calcium signaling via the chimeric protein Gαqi5 , 2009, Naunyn-Schmiedeberg's Archives of Pharmacology.

[70]  Hiroshi. Nakamura,et al.  Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally potent antianxiety drug. , 2009, Journal of medicinal chemistry.

[71]  T. Graczyk,et al.  Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859). , 2008, Journal of medicinal chemistry.

[72]  J. Neumeyer,et al.  Synthesis and pharmacological evaluation of hydrophobic esters and ethers of butorphanol at opioid receptors. , 2008, Bioorganic & medicinal chemistry letters.

[73]  D. Tulshian,et al.  The Anxiolytic-Like Effects of the Novel, Orally Active Nociceptin Opioid Receptor Agonist 8-[bis(2-Methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol (SCH 221510) , 2008, Journal of Pharmacology and Experimental Therapeutics.

[74]  David G. Lambert,et al.  The nociceptin/orphanin FQ receptor: a target with broad therapeutic potential , 2008, Nature Reviews Drug Discovery.

[75]  J. Cassel,et al.  Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor. , 2008, Bioorganic & medicinal chemistry letters.

[76]  S. Salvadori,et al.  Anxiolytic- and antidepressant-like activities of H-Dmt-Tic-NH-CH(CH2-COOH)-Bid (UFP-512), a novel selective delta opioid receptor agonist , 2008, Peptides.

[77]  アレキサンダー,ロベルタ,ヴェッザ,et al.  Synthetic peptide amides , 2007 .

[78]  K. Schiene,et al.  (–)-(1R,2R)-3-(3-Dimethylamino-1-ethyl-2-methyl-propyl)-phenol Hydrochloride (Tapentadol HCl): a Novel μ-Opioid Receptor Agonist/Norepinephrine Reuptake Inhibitor with Broad-Spectrum Analgesic Properties , 2007, Journal of Pharmacology and Experimental Therapeutics.

[79]  S. Salvadori,et al.  In vitro and in vivo studies on UFP-112, a novel potent and long lasting agonist selective for the nociceptin/orphanin FQ receptor , 2007, Peptides.

[80]  R. Ciccocioppo,et al.  Pharmacological Characterization of the Nociceptin/Orphanin FQ Receptor Antagonist SB-612111 [(–)-cis-1-Methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol]: In Vivo Studies , 2007, Journal of Pharmacology and Experimental Therapeutics.

[81]  D. Lambert,et al.  Pharmacological Characterization of the Nociceptin/Orphanin FQ Receptor Antagonist SB-612111 [(–)-cis-1-Methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol]: In Vitro Studies , 2007, Journal of Pharmacology and Experimental Therapeutics.

[82]  A. Basbaum,et al.  Knockin mice expressing fluorescent delta-opioid receptors uncover G protein-coupled receptor dynamics in vivo. , 2006, Proceedings of the National Academy of Sciences of the United States of America.

[83]  S. Salvadori,et al.  UFP-101, a peptide antagonist selective for the nociceptin/orphanin FQ receptor. , 2006, CNS drug reviews.

[84]  C. Tränkle,et al.  Cannabidiol is an allosteric modulator at mu- and delta-opioid receptors , 2006, Naunyn-Schmiedeberg's Archives of Pharmacology.

[85]  S. Salvadori,et al.  Identification of an achiral analogue of J-113397 as potent nociceptin/orphanin FQ receptor antagonist. , 2006, Bioorganic & medicinal chemistry.

[86]  Y. Iwasawa,et al.  Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity. , 2006, Journal of medicinal chemistry.

[87]  F. Heppner,et al.  Detection of kappa and delta opioid receptors in skin--outside the nervous system. , 2005, Biochemical and biophysical research communications.

[88]  E. Novellino,et al.  Syntheses, biological evaluation, and molecular modeling of 18F-labeled 4-anilidopiperidines as mu-opioid receptor imaging agents. , 2005, Journal of medicinal chemistry.

[89]  S. Salvadori,et al.  Blockade of Nociceptin/Orphanin FQ Transmission Attenuates Symptoms and Neurodegeneration Associated with Parkinson's Disease , 2005, The Journal of Neuroscience.

[90]  C. Woolf Faculty Opinions recommendation of Interaction with vesicle luminal protachykinin regulates surface expression of delta-opioid receptors and opioid analgesia. , 2005 .

[91]  G. Calo’,et al.  Functional Selectivity of Nociceptin/Orphanin FQ Peptide Receptor Partial Agonists on Cardiovascular and Renal Function , 2005, Journal of Pharmacology and Experimental Therapeutics.

[92]  T. F. Murray,et al.  [Nalpha-benzylTyr1,cyclo(D-Asp5,Dap8)]- dynorphin A-(1-11)NH2 cyclized in the "address" domain is a novel kappa-opioid receptor antagonist. , 2005, Journal of medicinal chemistry.

[93]  Cécile Béguin,et al.  Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2). , 2005, Bioorganic & medicinal chemistry letters.

[94]  J. Bidlack,et al.  Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone. , 2005, Bioorganic & medicinal chemistry letters.

[95]  M. Kreek,et al.  Pharmacogenetics and Human Molecular Genetics of Opiate and Cocaine Addictions and Their Treatments , 2005, Pharmacological Reviews.

[96]  T. Yeh,et al.  Heterodimerization of opioid receptor‐like 1 and µ‐opioid receptors impairs the potency of µ receptor agonist , 2005, Journal of neurochemistry.

[97]  S. Salvadori,et al.  [(pF)Phe4,Arg14,Lys15]N/OFQ-NH2 (UFP-102), a Highly Potent and Selective Agonist of the Nociceptin/Orphanin FQ Receptor , 2005, Journal of Pharmacology and Experimental Therapeutics.

[98]  S. Salvadori,et al.  N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands. , 2005, Journal of medicinal chemistry.

[99]  V. Höllt,et al.  Genetic disposition to addictive disorders--current knowledge and future perspectives. , 2005, Current opinion in pharmacology.

[100]  J. Lötsch,et al.  Are mu-opioid receptor polymorphisms important for clinical opioid therapy? , 2005, Trends in molecular medicine.

[101]  S. Schulz,et al.  Receptor Endocytosis Counteracts the Development of Opioid Tolerance , 2005, Molecular Pharmacology.

[102]  C. Abbadie,et al.  Immunohistochemical study of the expression of EXON11-containing μ opioid receptor variants in mouse brain , 2004, Neuroscience.

[103]  M. Narita,et al.  Increased level of neuronal phosphoinositide 3-kinase γ by the activation of μ-opioid receptor in the mouse periaqueductal gray matter: further evidence for the implication in morphine-induced antinociception , 2004, Neuroscience.

[104]  J. Ott,et al.  Redefinition of the human kappa opioid receptor gene (OPRK1) structure and association of haplotypes with opiate addiction. , 2004, Pharmacogenetics.

[105]  D. Kyle,et al.  Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor. , 2004, Bioorganic & medicinal chemistry letters.

[106]  R. Schulz,et al.  Opioid control of MAP kinase cascade. , 2004, European journal of pharmacology.

[107]  M. Zenk,et al.  Endogenous formation of morphine in human cells. , 2004, Proceedings of the National Academy of Sciences of the United States of America.

[108]  N. Mercuri,et al.  Blockade of Nociceptin/orphanin Fq Receptor Signaling in Rat Substantia Nigra Pars Reticulata Stimulates Nigrostriatal Dopaminergic Transmission and Motor Behavior ,lys 15 ]n/ofq(1–13)-nh 2 ) (a Selective Nop Receptor Peptide Antagonist) Stimulated It. N/ofq Microinjected in the Sub- Stantia Nigra P , 2022 .

[109]  L. Fan,et al.  Changes in acetylcholinesterase activity and muscarinic receptor bindings in mu-opioid receptor knockout mice. , 2004, Brain research. Molecular brain research.

[110]  B. Kieffer,et al.  Deficit in Attachment Behavior in Mice Lacking the µ-Opioid Receptor Gene , 2004, Science.

[111]  A. Beaudet,et al.  Mu-opioid receptor knockout prevents changes in delta-opioid receptor trafficking induced by chronic inflammatory pain , 2004, Pain.

[112]  K. Befort,et al.  The delta agonists DPDPE and deltorphin II recruit predominantly mu receptors to produce thermal analgesia: a parallel study of mu, delta and combinatorial opioid receptor knockout mice , 2004, The European journal of neuroscience.

[113]  Bryan L Roth,et al.  Salvinorin A, an Active Component of the Hallucinogenic Sage Salvia divinorum Is a Highly Efficacious κ-Opioid Receptor Agonist: Structural and Functional Considerations , 2004, Journal of Pharmacology and Experimental Therapeutics.

[114]  J. Miller,et al.  Abundant expression of mu and delta opioid receptor mRNA and protein in the cerebellum of the fetal, neonatal, and adult rat. , 2004, Brain research. Developmental brain research.

[115]  I. Sora,et al.  mu-Opioid receptor knockout mice display reduced cocaine conditioned place preference but enhanced sensitization of cocaine-induced locomotion. , 2004, Brain research. Molecular brain research.

[116]  M. Scheideler,et al.  Modification of Nociception and Morphine Tolerance by the Selective Opiate Receptor-Like Orphan Receptor Antagonist (–)-cis-1-Methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111) , 2004, Journal of Pharmacology and Experimental Therapeutics.

[117]  S. Kaasa,et al.  Genetic analysis of the murine μ opioid receptor: increased complexity of Oprm gene splicing , 2004, Journal of Molecular Medicine.

[118]  G. Pasternak,et al.  Functional analysis of MOR‐1 splice variants of the mouse mu opioid receptor gene Oprm , 2004, Synapse.

[119]  L. Ma,et al.  Chronic morphine treatment and withdrawal induce up-regulation of c-jun n-terminal kinase 3 gene expression in rat brain , 2003, Neuroscience.

[120]  S. Schulz,et al.  Heterodimerization of Substance P and μ-Opioid Receptors Regulates Receptor Trafficking and Resensitization* , 2003, Journal of Biological Chemistry.

[121]  K. Payza Binding and Activity of Opioid Ligands at the Cloned Human Delta, Mu, and Kappa Receptors , 2003 .

[122]  M. Narita,et al.  Reduced expression of a novel µ‐opioid receptor (MOR) subtype MOR‐1B in CXBK mice: Implications of MOR‐1B in the expression of MOR‐mediated responses , 2003, The European journal of neuroscience.

[123]  A. Beaudet,et al.  Phylogenetic changes in the expression of delta opioid receptors in spinal cord and dorsal root ganglia , 2003, The Journal of comparative neurology.

[124]  W Zieglgänsberger,et al.  [3h]-nociceptin ligand-binding and nociceptin opioid receptor mrna expression in the human brain , 2003, Neuroscience.

[125]  A. Forge,et al.  The opioid receptors in inner ear of different stages of postnatal rats , 2003, Hearing Research.

[126]  B. Kieffer,et al.  Basal and morphine‐evoked dopaminergic neurotransmission in the nucleus accumbens of MOR‐ and DOR‐knockout mice , 2003, The European journal of neuroscience.

[127]  Sabita Roy,et al.  Morphine Negatively Regulates Interferon-γ Promoter Activity in Activated Murine T Cells through Two Distinct Cyclic AMP-dependent Pathways* , 2003, Journal of Biological Chemistry.

[128]  H. Loh,et al.  Impaired water maze learning performance in mu-opioid receptor knockout mice. , 2003, Brain research. Molecular brain research.

[129]  J. Williams,et al.  Partial agonist behaviour depends upon the level of nociceptin/orphanin FQ receptor expression: studies using the ecdysone‐inducible mammalian expression system , 2003, British journal of pharmacology.

[130]  S. Allouche,et al.  Pharmacological characterization of AR-M1000390 at human delta opioid receptors. , 2003, Life sciences.

[131]  A. Forge,et al.  The presence of opioid receptors in rat inner ear , 2003, Hearing Research.

[132]  N. Zaveri Peptide and nonpeptide ligands for the nociceptin/orphanin FQ receptor ORL1: research tools and potential therapeutic agents. , 2003, Life sciences.

[133]  H. Loh,et al.  Differential effects of morphine and cocaine on locomotor activity and sensitization in μ-opioid receptor knockout mice , 2003, Neuroscience Letters.

[134]  H. Takeshima,et al.  Normal sensitivity to acute pain, but increased inflammatory hyperalgesia in mice lacking the nociceptin precursor polypeptide or the nociceptin receptor , 2003, The European journal of neuroscience.

[135]  C. Gaveriaux-Ruff,et al.  Anti-inflammatory properties of the mu opioid receptor support its use in the treatment of colon inflammation. , 2003, The Journal of clinical investigation.

[136]  H. Ueda,et al.  In Vivo Pain-Inhibitory Role of Nociceptin/Orphanin FQ in Spinal Cord , 2003, Journal of Pharmacology and Experimental Therapeutics.

[137]  R. Bertorelli,et al.  Blockade of nociceptin/orphanin FQ–NOP receptor signalling produces antidepressant‐like effects: pharmacological and genetic evidences from the mouse forced swimming test , 2003, The European journal of neuroscience.

[138]  J. Roder,et al.  Differential involvement of the Mu and Kappa opioid receptors in spatial learning , 2003, Genes, brain, and behavior.

[139]  Juei-Tang Cheng,et al.  Rapid induction of insulin resistance in opioid μ-receptor knock-out mice , 2003, Neuroscience Letters.

[140]  J. Pintar,et al.  Nociceptin/orphanin FQ knockout mice display up-regulation of the opioid receptor-like 1 receptor and alterations in opioid receptor expression in the brain , 2003, Neuroscience.

[141]  S. Schulz,et al.  ADP-ribosylation Factor-dependent Phospholipase D2 Activation Is Required for Agonist-induced μ-Opioid Receptor Endocytosis* , 2003, The Journal of Biological Chemistry.

[142]  R. Maldonado,et al.  Acute antinociceptive responses in single and combinatorial opioid receptor knockout mice: distinct mu, delta and kappa tones , 2003, The European journal of neuroscience.

[143]  D. Filliol,et al.  Enhanced humoral response in kappa-opioid receptor knockout mice , 2003, Journal of Neuroimmunology.

[144]  S. Hanessian,et al.  The power of visual imagery in drug design. Isopavines as a new class of morphinomimetics and their human opioid receptor binding activity. , 2003, Journal of medicinal chemistry.

[145]  D. Lambert,et al.  Pharmacological profiles of presynaptic nociceptin/orphanin FQ receptors modulating 5‐hydroxytryptamine and noradrenaline release in the rat neocortex , 2003, British journal of pharmacology.

[146]  A. Beaudet,et al.  Up-regulation and trafficking of δ opioid receptor in a model of chronic inflammation: implications for pain control , 2003, Pain.

[147]  M. Gunzer,et al.  Localization of μ-opioid receptor 1A on sensory nerve fibers in human skin , 2002, Regulatory Peptides.

[148]  L. Jan,et al.  Contribution of GIRK2-mediated postsynaptic signaling to opiate and α2-adrenergic analgesia and analgesic sex differences , 2002, Proceedings of the National Academy of Sciences of the United States of America.

[149]  R. Maldonado,et al.  Attenuation of Nicotine-Induced Antinociception, Rewarding Effects, and Dependence in μ-Opioid Receptor Knock-Out Mice , 2002, The Journal of Neuroscience.

[150]  De-Pei Li,et al.  Activation of delta-opioid receptors excites spinally projecting locus coeruleus neurons through inhibition of GABAergic inputs. , 2002, Journal of neurophysiology.

[151]  H. Akil,et al.  Expression of orphanin FQ and the opioid receptor-like (ORL1) receptor in the developing human and rat brain , 2002, Journal of Chemical Neuroanatomy.

[152]  J. Pintar,et al.  Autoradiography of opioid and ORL1 ligands in opioid receptor triple knockout mice , 2002, The European journal of neuroscience.

[153]  D. Filliol,et al.  Quantitative autoradiographic mapping of opioid receptors in the brain of δ-opioid receptor gene knockout mice , 2002, Brain Research.

[154]  G. Koob,et al.  Lack of reward and locomotor stimulation induced by heroin in mu-opioid receptor-deficient mice. , 2002, European journal of pharmacology.

[155]  T. Kenakin,et al.  G Protein-Coupled Receptor Allosterism and Complexing , 2002, Pharmacological Reviews.

[156]  S. Salvadori,et al.  [Nphe1,Arg14,Lys15]Nociceptin‐NH2, a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor , 2002, British journal of pharmacology.

[157]  S. Salvadori,et al.  Pharmacological characterisation of [(pX)Phe4]nociceptin(1-13)amide analogues , 2002, Naunyn-Schmiedeberg's Archives of Pharmacology.

[158]  C. Gaveriaux-Ruff,et al.  Opioid receptor genes inactivated in mice: the highlights , 2002, Neuropeptides.

[159]  Y. Wong,et al.  Co-Expressions of Different Opioid Receptor Types Differentially Modulate Their Signaling via G16 , 2002, Neurosignals.

[160]  H. Schroeder,et al.  Rewarding effects of ethanol and cocaine in µ opioid receptor-deficient mice , 2002, Naunyn-Schmiedeberg's Archives of Pharmacology.

[161]  I. Zagon,et al.  The biology of the opioid growth factor receptor (OGFr) , 2002, Brain Research Reviews.

[162]  L. Bohn,et al.  Mitogenic signaling via endogenous kappa-opioid receptors in C6 glioma cells: evidence for the involvement of protein kinase C and the mitogen-activated protein kinase signaling cascade. , 2001, Journal of neurochemistry.

[163]  G. Pasternak,et al.  Generation of the mu opioid receptor (MOR-1) protein by three new splice variants of the Oprm gene , 2001, Proceedings of the National Academy of Sciences of the United States of America.

[164]  L. Devi,et al.  G-protein-coupled receptor dimerization: modulation of receptor function. , 2001, Pharmacology & therapeutics.

[165]  D Horvath,et al.  From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands. , 2001, Journal of medicinal chemistry.

[166]  G. Pasternak,et al.  Differential in vivo internalization of MOR-1 and MOR-1C by morphine , 2001, Neuroreport.

[167]  W. Sadee,et al.  μ-Opioid Receptor-mediated ERK Activation Involves Calmodulin-dependent Epidermal Growth Factor Receptor Transactivation* , 2001, The Journal of Biological Chemistry.

[168]  G. Pasternak,et al.  The molecular and behavioral pharmacology of the orphanin FQ/nociceptin peptide and receptor family. , 2001, Pharmacological reviews.

[169]  V. Höllt,et al.  C-terminal Splice Variants of the Mouse μ-Opioid Receptor Differ in Morphine-induced Internalization and Receptor Resensitization* , 2001, The Journal of Biological Chemistry.

[170]  G. Beilman,et al.  Morphine directs T cells toward T(H2) differentiation. , 2001, Surgery.

[171]  F I Carroll,et al.  Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity. , 2001, Journal of medicinal chemistry.

[172]  T. Eisenstein,et al.  Opioids, opioid receptors, and the immune response. , 2001, Drug and alcohol dependence.

[173]  D. Filliol,et al.  A Single Nucleotide Polymorphic Mutation in the Human μ-Opioid Receptor Severely Impairs Receptor Signaling* , 2001, The Journal of Biological Chemistry.

[174]  I. Sora,et al.  Ethanol consumption and reward are decreased in µ-opiate receptor knockout mice , 2001, Psychopharmacology.

[175]  E. Valjent,et al.  Lack of dependence and rewarding effects of deltorphin II in mu‐opioid receptor‐deficient mice , 2001, The European journal of neuroscience.

[176]  G. Adam,et al.  Synthesis of (1S,3aS)-8- (2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaza-spiro [4.5]decan-4-one, a Potent and Selective Orphanin FQ (OFQ) Receptor Agonist with Anxiolytic-Like Properties. , 2000 .

[177]  A. Basbaum,et al.  Postsynaptic Signaling via the μ-Opioid Receptor: Responses of Dorsal Horn Neurons to Exogenous Opioids and Noxious Stimulation , 2000, The Journal of Neuroscience.

[178]  Y. Yamada,et al.  Highly potent nociceptin analog containing the Arg-Lys triple repeat. , 2000, Biochemical and biophysical research communications.

[179]  L. Devi,et al.  Heterodimerization of mu and delta opioid receptors: A role in opiate synergy. , 2000, The Journal of neuroscience : the official journal of the Society for Neuroscience.

[180]  H. Yamada,et al.  4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. , 2000, Journal of medicinal chemistry.

[181]  H. Ueda,et al.  Enhanced Spinal Nociceptin Receptor Expression Develops Morphine Tolerance and Dependence , 2000, The Journal of Neuroscience.

[182]  J. Costentin,et al.  Autoradiographic localization of [3H]nociceptin binding sites in the rat brain , 2000, Brain Research.

[183]  G. Adam,et al.  Synthesis of (1S,3aS)-8-(2,3,3a,4,5, 6-hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaza-spiro[4. 5]decan-4-one, a potent and selective orphanin FQ (OFQ) receptor agonist with anxiolytic-like properties. , 2000, European journal of medicinal chemistry.

[184]  B. O'dowd,et al.  Oligomerization of mu- and delta-opioid receptors. Generation of novel functional properties. , 2000, The Journal of biological chemistry.

[185]  Y. Iwasawa,et al.  In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL1 receptor antagonist. , 2000, European journal of pharmacology.

[186]  T. Kroslak,et al.  Allelic variation S268P of the human mu-opioid receptor affects both desensitization and G protein coupling. , 2000, Molecular pharmacology.

[187]  S. Salvadori,et al.  Nociceptin/orphanin FQ receptor ligands , 2000, Peptides.

[188]  C. Topham,et al.  The nociceptin (ORL1) receptor: molecular cloning and functional architecture , 2000, Peptides.

[189]  L. Moulédous,et al.  Tissue distribution of the opioid receptor-like (ORL1) receptor , 2000, Peptides.

[190]  B. Hawes,et al.  Cellular actions of nociceptin: transduction mechanisms , 2000, Peptides.

[191]  R. M. Jones,et al.  Potent and selective indolomorphinan antagonists of the kappa-opioid receptor. , 2000, Journal of medicinal chemistry.

[192]  H. Schroeder,et al.  Morphine self-administration in µ-opioid receptor-deficient mice , 2000, Naunyn-Schmiedeberg's Archives of Pharmacology.

[193]  M. Krug,et al.  Lack of expression of long-term potentiation in the dentate gyrus but not in the CA1 region of the hippocampus of μ-opioid receptor-deficient mice , 2000, Neuropharmacology.

[194]  G. Adam,et al.  A synthetic agonist at the orphanin FQ/nociceptin receptor ORL1: anxiolytic profile in the rat. , 2000, Proceedings of the National Academy of Sciences of the United States of America.

[195]  G. Pasternak,et al.  Differential distribution in rat brain of mu opioid receptor carboxy terminal splice variants MOR‐1C‐like and MOR‐1‐like immunoreactivity: Evidence for region‐specific processing , 2000, The Journal of comparative neurology.

[196]  S. Salvadori,et al.  Characterization of [Nphe1]nociceptin(1‐13)NH2, a new selective nociceptin receptor antagonist , 2000, British journal of pharmacology.

[197]  J. Menzies,et al.  In vitro agonist effects of nociceptin and [Phe(1)psi(CH(2)-NH)Gly(2)]nociceptin(1-13)NH(2) in the mouse and rat colon and the mouse vas deferens. , 1999, European journal of pharmacology.

[198]  I. Zagon,et al.  Cloning, sequencing, expression and function of a cDNA encoding a receptor for the opioid growth factor, [Met5]enkephalin 1 The nucleotide sequence of the rat OGFr has been deposited in GenBank under accession number AF 156878. 1 , 1999, Brain Research.

[199]  Y. Iwasawa,et al.  Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl-1, 3-dihydro-2H-benzimidazol-2-one (J-113397). , 1999, Journal of medicinal chemistry.

[200]  D. Richter,et al.  Reverse physiology in Drosophila: identification of a novel allatostatin‐like neuropeptide and its cognate receptor structurally related to the mammalian somatostatin/galanin/opioid receptor family , 1999, The EMBO journal.

[201]  H. Masuda,et al.  Modification of acetylcholine release by nociceptin in conscious rat striatum , 1999, Brain Research.

[202]  H. Akil,et al.  Opioid receptor‐like (ORL1) receptor distribution in the rat central nervous system: Comparison of ORL1 receptor mRNA expression with 125I‐[14Tyr]‐orphanin FQ binding , 1999, The Journal of comparative neurology.

[203]  D. Kapusta,et al.  Cardiovascular and renal responses produced by central orphanin FQ/nociceptin occur independent of renal nerves. , 1999, American journal of physiology. Regulatory, integrative and comparative physiology.

[204]  H. Ueda,et al.  Dose-related opposite modulation by nociceptin/orphanin FQ of substance P nociception in the nociceptors and spinal cord. , 1999, The Journal of pharmacology and experimental therapeutics.

[205]  F. Simonin,et al.  Ligands for κ-Opioid and ORL1 Receptors Identified from a Conformationally Constrained Peptide Combinatorial Library* , 1999, The Journal of Biological Chemistry.

[206]  A. Loizzo,et al.  Orphanin FQ reduces morphine-induced dopamine release in the nucleus accumbens: a microdialysis study in rats , 1999, Neuroscience Letters.

[207]  Joshua F. Nitsche,et al.  Retention of Supraspinal Delta-like Analgesia and Loss of Morphine Tolerance in δ Opioid Receptor Knockout Mice , 1999, Neuron.

[208]  G. Adam,et al.  8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists. , 1999, Bioorganic & medicinal chemistry letters.

[209]  M. Connor,et al.  OPIOID RECEPTOR SIGNALLING MECHANISMS , 1999, Clinical and experimental pharmacology & physiology.

[210]  Pll Siinksen,et al.  Control , 1999, Netherlands Journal of Plant Pathology.

[211]  D. Lambert,et al.  Comparison of the effects of [Phe1Ψ(CH2‐NH)Gly2]Nociceptin (1–13)NH2 in rat brain, rat vas deferens and CHO cells expressing recombinant human nociceptin receptors , 1999, British journal of pharmacology.

[212]  J. Pintar,et al.  μ‐opioid receptor modulation of calcium channel current in periaqueductal grey neurons from C57B16/J mice and mutant mice lacking MOR‐1 , 1999, British journal of pharmacology.

[213]  C. Maggi,et al.  Characterization of nociceptin receptors in the periphery: in vitro and in vivo studies , 1999, Naunyn-Schmiedeberg's Archives of Pharmacology.

[214]  H. Akil,et al.  Opioid efficacy in a C6 glioma cell line stably expressing the human kappa opioid receptor. , 1999, The Journal of pharmacology and experimental therapeutics.

[215]  D. Peckys,et al.  Expression of mu, kappa, and delta opioid receptor messenger RNA in the human CNS: a 33P in situ hybridization study , 1999, Neuroscience.

[216]  Shengwen Zhang,et al.  Endomorphins fully activate a cloned human mu opioid receptor , 1998, FEBS letters.

[217]  H. Loh,et al.  MU-opioid receptor-knockout mice: role of μ-opioid receptor in morphine mediated immune functions , 1998 .

[218]  M. Kathmann,et al.  Nociceptin inhibits noradrenaline release in the mouse brain cortex via presynaptic ORL1 receptors , 1998, Naunyn-Schmiedeberg's Archives of Pharmacology.

[219]  J. Pintar,et al.  Expression of opioid receptors and ligands in pregnant mouse uterus and placenta. , 1998, Biology of reproduction.

[220]  H. Ueda,et al.  Nociceptin/orphanin FQ-induced nociceptive responses through substance P release from peripheral nerve endings in mice. , 1998, Proceedings of the National Academy of Sciences of the United States of America.

[221]  T. Manabe,et al.  Facilitation of long-term potentiation and memory in mice lacking nociceptin receptors , 1998, Nature.

[222]  J A Tischfield,et al.  Single-nucleotide polymorphism in the human mu opioid receptor gene alters beta-endorphin binding and activity: possible implications for opiate addiction. , 1998, Proceedings of the National Academy of Sciences of the United States of America.

[223]  T. Kaneko,et al.  Immunocytochemical localization of μ-opioid receptor in primary afferent neurons containing substance P or calcitonin gene-related peptide. A light and electron microscope study in the rat , 1998, Brain Research.

[224]  S. Schulz,et al.  Carboxyl-terminal Splicing of the Rat μ Opioid Receptor Modulates Agonist-mediated Internalization and Receptor Resensitization* , 1998, The Journal of Biological Chemistry.

[225]  H. Matthes,et al.  Abolition of morphine-immunosuppression in mice lacking the mu-opioid receptor gene. , 1998, Proceedings of the National Academy of Sciences of the United States of America.

[226]  B. Ashby,et al.  Agonist-induced desensitization and down-regulation of the human kappa opioid receptor expressed in Chinese hamster ovary cells. , 1998, The Journal of pharmacology and experimental therapeutics.

[227]  H. Masuda,et al.  Modification of dopamine release by nociceptin in conscious rat striatum , 1998, Brain Research.

[228]  Yoshihiro Yoshihara,et al.  Nocistatin, a peptide that blocks nociceptin action in pain transmission , 1998, Nature.

[229]  Sabita Roy,et al.  Evidence for opioid receptors on cells involved in host defense and the immune system , 1998, Journal of Neuroimmunology.

[230]  A. Cavalli,et al.  mu Opioid receptor knockout in mice: effects on ligand-induced analgesia and morphine lethality. , 1998, Brain research. Molecular brain research.

[231]  J. M. Kennedy,et al.  Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications. , 1998, NIDA research monograph.

[232]  B. Roques,et al.  Disruption of the κ‐opioid receptor gene in mice enhances sensitivity to chemical visceral pain, impairs pharmacological actions of the selective κ‐agonist U‐50,488H and attenuates morphine withdrawal , 1998, The EMBO journal.

[233]  S. Salvadori,et al.  A new selective antagonist of the nociceptin receptor , 1998, British journal of pharmacology.

[234]  F. Monsma,et al.  Orphanin FQ acts as an anxiolytic to attenuate behavioral responses to stress. , 1997, Proceedings of the National Academy of Sciences of the United States of America.

[235]  P. Szekeres,et al.  Delta opioid modulation of the binding of guanosine-5'-O-(3-[35S]thio)triphosphate to NG108-15 cell membranes: characterization of agonist and inverse agonist effects. , 1997, The Journal of pharmacology and experimental therapeutics.

[236]  D. Mangoura,et al.  μ‐Opioids activate tyrosine kinase focal adhesion kinase and regulate cortical cytoskeleton proteins cortactin and vinculin in chick embryonic neurons , 1997, Journal of neuroscience research.

[237]  R. Houghten,et al.  Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1. , 1997, The Journal of pharmacology and experimental therapeutics.

[238]  L. Devi,et al.  Dimerization of the delta opioid receptor: implication for a role in receptor internalization. , 1997, The Journal of biological chemistry.

[239]  S. Schulz,et al.  Immunolocalization of two mu-opioid receptor isoforms (MOR1 and MOR1B) in the rat central nervous system , 1997, Neuroscience.

[240]  L. Toll,et al.  Relationship between binding affinity and functional activity of nociceptin/orphanin FQ , 1997, Neuropeptides.

[241]  V. Pickel,et al.  Ultrastructural immunocytochemical localization of μ-opioid receptors in dendritic targets of dopaminergic terminals in the rat caudate–putamen nucleus , 1997, Neuroscience.

[242]  H. Akil,et al.  Cellular localization and distribution of the cloned mu and kappa opioid receptors in rat gastrointestinal tract , 1997, Neuroscience.

[243]  J. Li,et al.  Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands. , 1997, The Journal of pharmacology and experimental therapeutics.

[244]  S. Salvadori,et al.  Address and message sequences for the nociceptin receptor: a structure-activity study of nociceptin-(1-13)-peptide amide. , 1997, Journal of medicinal chemistry.

[245]  H. Jansen,et al.  Altered Hematopoiesis, Behavior, and Sexual Function in μ Opioid Receptor–deficient Mice , 1997, The Journal of experimental medicine.

[246]  J. Kuno,et al.  Unrestrained nociceptive response and disregulation of hearing ability in mice lacking the nociceptin/orphaninFQ receptor , 1997, The EMBO journal.

[247]  I. Sora,et al.  The mu-opioid receptor is necessary for [D-Pen2,D-Pen5]enkephalin-induced analgesia. , 1997, European journal of pharmacology.

[248]  Z. Vogel,et al.  Opiate-induced Adenylyl Cyclase Superactivation Is Isozyme-specific* , 1997, The Journal of Biological Chemistry.

[249]  I. Sora,et al.  Opiate receptor knockout mice define mu receptor roles in endogenous nociceptive responses and morphine-induced analgesia. , 1997, Proceedings of the National Academy of Sciences of the United States of America.

[250]  E. V. Van Bockstaele,et al.  Mu‐opioid receptor is located on the plasma membrane of dendrites that receive asymmetric synapses from axon terminals containing leucine‐enkephalin in the rat nucleus locus coeruleus , 1996, The Journal of comparative neurology.

[251]  P B Bradley,et al.  International Union of Pharmacology. XII. Classification of opioid receptors. , 1996, Pharmacological reviews.

[252]  D. Lambert,et al.  Nociceptin induced inhibition of K+ evoked glutamate release from rat cerebrocortical slices , 1996, British journal of pharmacology.

[253]  B. O'dowd,et al.  Agonist-induced functional desensitization of the mu-opioid receptor is mediated by loss of membrane receptors rather than uncoupling from G protein. , 1996, Molecular pharmacology.

[254]  Brigitte L. Kieffer,et al.  Loss of morphine-induced analgesia, reward effect and withdrawal symptoms in mice lacking the µ-opioid-receptor gene , 1996, Nature.

[255]  M. Parmentier,et al.  Replacement of Gln280 by His in TM6 of the human ORL1 receptor increases affinity but reduces intrinsic activity of opioids , 1996, FEBS letters.

[256]  G. Gebhart,et al.  Kappa, but not mu or delta, opioids attenuate responses to distention of afferent fibers innervating the rat colon. , 1996, Gastroenterology.

[257]  T. Schwartz,et al.  Radioligand-dependent discrepancy in agonist affinities enhanced by mutations in the kappa-opioid receptor. , 1996, Molecular pharmacology.

[258]  G. Makhlouf,et al.  Opioid mu, delta, and kappa receptor-induced activation of phospholipase C-beta 3 and inhibition of adenylyl cyclase is mediated by Gi2 and G(o) in smooth muscle. , 1996, Molecular pharmacology.

[259]  A. Pande,et al.  Analgesic efficacy of enadoline versus placebo or morphine in postsurgical pain. , 1996, Clinical neuropharmacology.

[260]  T. Hales,et al.  Voltage-dependent inhibition of Ca2+ channels in GH3 cells by cloned mu- and delta-opioid receptors. , 1996, Molecular pharmacology.

[261]  N. Maidment,et al.  Intracerebroventricular orphanin FQ/Nociceptin supresses dopamine release in the nucleus accumbens of anaesthetized rats , 1996, Neuroscience.

[262]  V. Neugebauer,et al.  The mouse vas deferens: a pharmacological preparation sensitive to nociceptin. , 1996, European journal of pharmacology.

[263]  Xiao-jun Xu,et al.  Nociceptin or antinociceptin: potent spinal antinociceptive effect of orphanin FQ/nociceptin in the rat. , 1996, Neuroreport.

[264]  D. Grandy,et al.  Orphanin FQ acts as a supraspinal, but not a spinal, anti‐opioid peptide , 1996, Neuroreport.

[265]  K. Chang,et al.  The stimulatory effect of opioids on mitogen-activated protein kinase in Chinese hamster ovary cells transfected to express mu-opioid receptors. , 1996, Molecular pharmacology.

[266]  B. Chieng,et al.  The mu-opioid receptor antagonist D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP) [but not D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2 (CTAP)] produces a nonopioid receptor-mediated increase in K+ conductance of rat locus ceruleus neurons. , 1996, Molecular pharmacology.

[267]  V. Pickel,et al.  Ultrastructural localization of μ-opioid receptors in the superficial layers of the rat cervical spinal cord: extrasynaptic localization and proximity to Leu5-enkephalin , 1996, Brain Research.

[268]  V. Pickel,et al.  Ultrastructural Evidence for Prominent Distribution of the μ-Opioid Receptor at Extrasynaptic Sites on Noradrenergic Dendrites in the Rat Nucleus Locus Coeruleus , 1996, The Journal of Neuroscience.

[269]  M. Parmentier,et al.  Structure, tissue distribution, and chromosomal localization of the prepronociceptin gene. , 1996, Proceedings of the National Academy of Sciences of the United States of America.

[270]  K. Shark,et al.  kappa opioid receptors in human microglia downregulate human immunodeficiency virus 1 expression. , 1996, Proceedings of the National Academy of Sciences of the United States of America.

[271]  E. Kempner,et al.  Purification, molecular cloning, and expression of the mammalian sigma1-binding site. , 1996, Proceedings of the National Academy of Sciences of the United States of America.

[272]  V. Pickel,et al.  Ultrastructural Immunocytochemical Localization of μ-Opioid Receptors in Rat Nucleus Accumbens: Extrasynaptic Plasmalemmal Distribution and Association with Leu5-Enkephalin , 1996, The Journal of Neuroscience.

[273]  B. Tabakoff,et al.  mu-Opioid receptors inhibit dopamine-stimulated activity of type V adenylyl cyclase but enhance dopamine-stimulated activity of type VII adenylyl cyclase. , 1996, Molecular pharmacology.

[274]  A. Zimprich,et al.  Promoter Region and Alternatively Spliced Exons of the Rat μ‐Opioid Receptor Gene , 1996, Journal of neurochemistry.

[275]  M. Connor,et al.  The effect of nociceptin on Ca2+ channel current and intracellular Ca2+ in the SH‐SY5Y human neuroblastoma cell line , 1996, British journal of pharmacology.

[276]  L. Toll,et al.  Determination of activity for nociceptin in the mouse vas deferens. , 1996, European journal of pharmacology.

[277]  T. Vanderah,et al.  Opioid receptor types and subtypes: the delta receptor as a model. , 1996, Annual review of pharmacology and toxicology.

[278]  T. Soong,et al.  Determinants of the G protein-dependent opioid modulation of neuronal calcium channels. , 1996, Proceedings of the National Academy of Sciences of the United States of America.

[279]  S. Husbands,et al.  Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group: High affinity opioid agonists , 1995 .

[280]  Brigitte L. Kieffer,et al.  Recent advances in molecular recognition and signal transduction of active peptides: Receptors for opioid peptides , 1995, Cellular and Molecular Neurobiology.

[281]  Y. Wong,et al.  Activation of Type II Adenylyl Cyclase by the Cloned μ‐Opioid Receptor: Coupling to Multiple G Proteins , 1995, Journal of neurochemistry.

[282]  H. Kung,et al.  Mu opioid receptor gene expression in immune cells. , 1995, Biochemical and biophysical research communications.

[283]  D. Grandy,et al.  Orphanin FQ: A Neuropeptide That Activates an Opioidlike G Protein-Coupled Receptor , 1995, Science.

[284]  T. Kaneko,et al.  Presynaptic localization of μ-opioid receptor-like immunoreactivity in retinal axon terminals within the terminal nuclei of the accessory optic tract: a light and electron microscope study in the rat , 1995, Neuroscience Letters.

[285]  M. Dapoigny,et al.  Efficacy of peripheral kappa agonist fedotozine versus placebo in treatment of irritable bowel syndrome , 1995, Digestive Diseases and Sciences.

[286]  T. Kaneko,et al.  Co-localization of μ-opioid receptor-like and substance P-like immunoreactivities in axon terminals within the superficial layers of the medullary and spinal dorsal horns of the rat , 1995, Neuroscience Letters.

[287]  D. Selley,et al.  In vitro autoradiography of receptor-activated G proteins in rat brain by agonist-stimulated guanylyl 5'-[gamma-[35S]thio]-triphosphate binding. , 1995, Proceedings of the National Academy of Sciences of the United States of America.

[288]  B. Bloch,et al.  kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system. , 1995, Proceedings of the National Academy of Sciences of the United States of America.

[289]  A. I. Brooks,et al.  Cloning and functional characterization through antisense mapping of a kappa 3-related opioid receptor. , 1995, Molecular pharmacology.

[290]  S. D. Glick,et al.  Kappa opioid inhibition of morphine and cocaine self-administration in rats , 1995, Brain Research.

[291]  H. Loh,et al.  The kappa-opioid receptor is primarily postsynaptic: combined immunohistochemical localization of the receptor and endogenous opioids. , 1995, Proceedings of the National Academy of Sciences of the United States of America.

[292]  H. Loh,et al.  Distribution and targeting of a mu-opioid receptor (MOR1) in brain and spinal cord , 1995, The Journal of neuroscience : the official journal of the Society for Neuroscience.

[293]  H. Loh,et al.  Ca2+ channel and adenylyl cyclase modulation by cloned mu-opioid receptors in GH3 cells. , 1995, Molecular Pharmacology.

[294]  Z. Vogel,et al.  κ‐Opioid receptor‐transfected cell lines: modulation of adenylyl cyclase activity following acute and chronic opioid treatments , 1995, FEBS letters.

[295]  D. Grandy,et al.  Kappa-opioid receptors couple to inwardly rectifying potassium channels when coexpressed by Xenopus oocytes. , 1995, Molecular pharmacology.

[296]  Stanley J. Watson,et al.  Opioid-receptor mRNA expression in the rat CNS: anatomical and functional implications , 1995, Trends in Neurosciences.

[297]  T. Kaneko,et al.  Immunocytochemical localization of μ-opioid receptor in the rat caudate-putamen , 1995, Neuroscience Letters.

[298]  C. Lupica Delta and mu enkephalins inhibit spontaneous GABA-mediated IPSCs via a cyclic AMP-independent mechanism in the rat hippocampus , 1995, The Journal of neuroscience : the official journal of the Society for Neuroscience.

[299]  B. O'dowd,et al.  Distinct distributions of mu, delta and kappa opioid receptor mRNA in rat brain. , 1994, Biochemical and biophysical research communications.

[300]  M. Nishi,et al.  Structure and chromosomal mapping of genes for the mouse kappa-opioid receptor and an opioid receptor homologue (MOR-C). , 1994, Biochemical and biophysical research communications.

[301]  M. Dichter,et al.  The cloned kappa opioid receptor couples to an N-type calcium current in undifferentiated PC-12 cells , 1994, Neuroscience.

[302]  H. Rhim,et al.  Opioid receptors modulate diverse types of calcium channels in the nucleus tractus solitarius of the rat , 1994, The Journal of neuroscience : the official journal of the Society for Neuroscience.

[303]  H. Matthes,et al.  The human delta-opioid receptor: genomic organization, cDNA cloning, functional expression, and distribution in human brain. , 1994, Molecular pharmacology.

[304]  R. Macdonald,et al.  Mu- and kappa-opioid receptors selectively reduce the same transient components of high-threshold calcium current in rat dorsal root ganglion sensory neurons , 1994, The Journal of neuroscience : the official journal of the Society for Neuroscience.

[305]  H. Loh,et al.  Genomic structure analysis of promoter sequence of a mouse mu opioid receptor gene. , 1994, Proceedings of the National Academy of Sciences of the United States of America.

[306]  J. Flippen-Anderson,et al.  Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist. , 1994, Journal of medicinal chemistry.

[307]  B. Ozenberger,et al.  cDNA Cloning of an orphan opiate receptor gene family member and its splice variant , 1994, FEBS letters.

[308]  A. Ohnishi,et al.  Aquaretic effect of the stable dynorphin-A analog E2078 in the human. , 1994, The Journal of pharmacology and experimental therapeutics.

[309]  M. Chesselet,et al.  Expression of Mu opioid receptor mRNA in rat brain: An in situ hybridization study at the single cell level , 1994, The Journal of comparative neurology.

[310]  P. Rubin,et al.  The cardiovascular and central nervous system effects in the human of U-62066E , 1994, European Journal of Clinical Pharmacology.

[311]  R. Gottschlich,et al.  EMD 61 753 as a favourable representative of structurally novel arylacetamido-type K opiate receptor agonists , 1994 .

[312]  L. Urbán,et al.  Opioids suppress spontaneous activity of polymodal nociceptors in rat paw skin induced by ultraviolet irradiation , 1994, Neuroscience.

[313]  G. Bell,et al.  Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors. , 1994, Molecular pharmacology.

[314]  G. Uhl,et al.  Human mu opiate receptor. cDNA and genomic clones, pharmacologic characterization and chromosomal assignment. , 1994, FEBS letters.

[315]  J. Williams,et al.  kappa-Opioid receptors also increase potassium conductance. , 1993, Proceedings of the National Academy of Sciences of the United States of America.

[316]  A Goldstein,et al.  Cloning and pharmacological characterization of a rat kappa opioid receptor. , 1993, Proceedings of the National Academy of Sciences of the United States of America.

[317]  Stanley J. Watson,et al.  Cloning and pharmacological characterization of a rat μ opioid receptor , 1993, Neuron.

[318]  Robert C. Thompson,et al.  Delta opioid receptor mRNA distribution in the brain: Comparison to delta receptor binding and proenkephalin mRNA , 1993, Journal of Chemical Neuroanatomy.

[319]  C. Chen,et al.  Molecular cloning and expression of a rat kappa opioid receptor. , 1993, The Biochemical journal.

[320]  Y. Chen,et al.  Molecular cloning of a rat kappa opioid receptor reveals sequence similarities to the mu and delta opioid receptors. , 1993, The Biochemical journal.

[321]  G. Uhl,et al.  mu opiate receptor: cDNA cloning and expression. , 1993, Proceedings of the National Academy of Sciences of the United States of America.

[322]  J. L. Howard,et al.  A novel, potent and selective nonpeptidic delta opioid receptor agonist BW373U86. , 1993, The Journal of pharmacology and experimental therapeutics.

[323]  P. Schiller,et al.  TIPP[psi]: a highly potent and stable pseudopeptide delta opioid receptor antagonist with extraordinary delta selectivity. , 1993, Journal of medicinal chemistry.

[324]  K. Mori,et al.  cDNA cloning and pharmacological characterization of an opioid receptor with high affinities for κ‐subtype‐selective ligands , 1993, FEBS letters.

[325]  J. Bidlack,et al.  The kappa opioid receptor expressed on the mouse R1.1 thymoma cell line is coupled to adenylyl cyclase through a pertussis toxin-sensitive guanine nucleotide-binding regulatory protein. , 1993, The Journal of pharmacology and experimental therapeutics.

[326]  F. Porreca,et al.  Differential antagonism of bremazocine- and U69,593-induced antinociception by quadazocine: further functional evidence of opioid kappa receptor multiplicity in the mouse. , 1993, The Journal of pharmacology and experimental therapeutics.

[327]  G. Bell,et al.  Cloning and functional comparison of kappa and delta opioid receptors from mouse brain. , 1993, Proceedings of the National Academy of Sciences of the United States of America.

[328]  Lei Yu,et al.  Molecular cloning and functional expression of a mu opioid receptor from rat brain , 1994, Regulatory Peptides.

[329]  B. Carter,et al.  Go mediates the coupling of the mu opioid receptor to adenylyl cyclase in cloned neural cells and brain. , 1993, Proceedings of the National Academy of Sciences of the United States of America.

[330]  S. Childers,et al.  Relationship between kappa 1 opioid receptor binding and inhibition of adenylyl cyclase in guinea pig brain membranes. , 1993, Biochemical pharmacology.

[331]  R. Edwards,et al.  Cloning of a delta opioid receptor by functional expression. , 1992, Science.

[332]  T. Hughes,et al.  Binding and pharmacological evidence for a special subtype of delta opioid receptor on human and invertebrate immune cells , 1992, Journal of Neuroimmunology.

[333]  C. Xie,et al.  Mu opioid receptor-mediated modulation of synaptic currents in dentate granule cells of rat hippocampus. , 1992, Journal of neurophysiology.

[334]  D. Ann,et al.  Specific reduction of delta-opioid receptor binding in transfected NG108-15 cells. , 1992, Journal of Biological Chemistry.

[335]  P. Rubin,et al.  Mechanism of diuretic action of spiradoline (U-62066E)--a kappa opioid receptor agonist in the human. , 1991, British journal of clinical pharmacology.

[336]  F. Porreca,et al.  Differential antagonism of U69,593- and bremazocine-induced antinociception by (-)-UPHIT: evidence of kappa opioid receptor multiplicity in mice. , 1991, The Journal of pharmacology and experimental therapeutics.

[337]  P. Portoghese,et al.  Differential antagonism of delta opioid agonists by naltrindole and its benzofuran analog (NTB) in mice: evidence for delta opioid receptor subtypes. , 1991, The Journal of pharmacology and experimental therapeutics.

[338]  D. Taub,et al.  Immunomodulatory activity of mu- and kappa-selective opioid agonists. , 1991, Proceedings of the National Academy of Sciences of the United States of America.

[339]  R. Spanagel,et al.  The Effects of Opioid Peptides on Dopamine Release in the Nucleus Accumbens: An In Vivo Microdialysis Study , 1990, Journal of neurochemistry.

[340]  W. Sadee,et al.  Regulation of Cyclic AMP by the μ‐Opioid Receptor in Human Neuroblastoma SH‐SY5Y Cells , 1990, Journal of neurochemistry.

[341]  D. Rees,et al.  CI‐977, a novel and selective agonist for the κ‐opioid receptor , 1990, British journal of pharmacology.

[342]  A Herz,et al.  Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. , 1989, Proceedings of the National Academy of Sciences of the United States of America.

[343]  A. Goldstein,et al.  Multiple opioid receptors: ligand selectivity profiles and binding site signatures. , 1989, Molecular pharmacology.

[344]  D. Barra,et al.  Deltorphins: a family of naturally occurring peptides with high affinity and selectivity for delta opioid binding sites. , 1989, Proceedings of the National Academy of Sciences of the United States of America.

[345]  N. Sharif,et al.  Discrete mapping of brain mu and delta opioid receptors using selective peptides: Quantitative autoradiography, species differences and comparison with kappa receptors , 1989, Peptides.

[346]  T. Shippenberg,et al.  Peripheral opioid receptors mediating antinociception in inflammation. Evidence for involvement of mu, delta and kappa receptors. , 1989, The Journal of pharmacology and experimental therapeutics.

[347]  K. Rice,et al.  Selective and enantiospecific acylation of kappa opioid receptors by (1S,2S)-trans-2-isothiocyanato-N-methyl-N-[2-(1-pyrrolidinyl) cyclohexy l] benzeneacetamide. Demonstration of kappa receptor heterogeneity. , 1989, Journal of medicinal chemistry.

[348]  T. Blackburn,et al.  Autoradiographic localization of delta opiate receptors in rat and human brain , 1988, Neuroscience.

[349]  A. Cowan,et al.  Role of Opioid Receptors in Bombesin‐induced Grooming a , 1988, Annals of the New York Academy of Sciences.

[350]  B. Roques,et al.  [3H][D-Ser2(O-tert-butyl),Leu5]enkephalyl-Thr6 and [D-Ser2(O-tert-butyl),Leu5]enkephalyl-Thr6(O-tert-butyl). Two new enkephalin analogs with both a good selectivity and a high affinity toward delta-opioid binding sites. , 1988, The Journal of biological chemistry.

[351]  G. Di Chiara,et al.  Opposite effects of mu and kappa opiate agonists on dopamine release in the nucleus accumbens and in the dorsal caudate of freely moving rats. , 1988, The Journal of pharmacology and experimental therapeutics.

[352]  D. L. Larson,et al.  Hybrid bivalent ligands with opiate and enkephalin pharmacophores. , 1987, Journal of medicinal chemistry.

[353]  H. Akil,et al.  Autoradiographic differentiation of mu, delta, and kappa opioid receptors in the rat forebrain and midbrain , 1987 .

[354]  J T Williams,et al.  Mu and delta receptors belong to a family of receptors that are coupled to potassium channels. , 1987, Proceedings of the National Academy of Sciences of the United States of America.

[355]  R. Zukin,et al.  Neuroanatomical patterns of the mu, delta, and kappa opioid receptors of rat brain as determined by quantitative in vitro autoradiography. , 1987, Proceedings of the National Academy of Sciences of the United States of America.

[356]  K. Gulya,et al.  Autoradiographic localization of [3H] [MePhe3,D-Pro4]morphiceptin ([3H]PL017) to mu opioid receptors in rat brain. , 1987, European journal of pharmacology.

[357]  A. Pfeiffer,et al.  Effects of a kappa-opioid agonist on adrenocorticotropic and diuretic function in man. , 1986, Hormone and metabolic research = Hormon- und Stoffwechselforschung = Hormones et metabolisme.

[358]  V. Hruby,et al.  Cyclic somatostatin octapeptide analogues with high affinity and selectivity toward mu opioid receptors. , 1986, Life sciences.

[359]  D. Zichi,et al.  Factors affecting binding of trans-N-[2-(methylamino)cyclohexyl]benzamides at the primary morphine receptor. , 1985, Journal of medicinal chemistry.

[360]  V. Hruby,et al.  Characterization of [3H][2-D-penicillamine, 5-D-penicillamine]-enkephalin binding to delta opiate receptors in the rat brain and neuroblastoma--glioma hybrid cell line (NG 108-15). , 1985, Proceedings of the National Academy of Sciences of the United States of America.

[361]  H. Loh,et al.  Multiple affinity states of opiate receptor in neuroblastoma x glioma NG108-15 hybrid cells. Opiate agonist association rate is a function of receptor occupancy. , 1985, The Journal of biological chemistry.

[362]  J. Leander Kappa Opioid Agonists and Antagonists: Effects on Drinking and Urinary Output , 1984, Appetite.

[363]  J. K. Chang,et al.  Potent morphiceptin analogs: structure activity relationships and morphine-like activities. , 1983, The Journal of pharmacology and experimental therapeutics.

[364]  T F Burks,et al.  Bis-penicillamine enkephalins possess highly improved specificity toward delta opioid receptors. , 1983, Proceedings of the National Academy of Sciences of the United States of America.

[365]  A. Korczyn,et al.  The pupillary effects of opioids. , 1983, Life sciences.

[366]  A. Tavani,et al.  The binding spectrum of narcotic analgesic drugs with different agonist and antagonist properties , 1982, Naunyn-Schmiedeberg's Archives of Pharmacology.

[367]  J. H. Ludens,et al.  Studies on the nature and mechanism of the diuretic activity of the opioid analgesic ethylketocyclazocine. , 1982, The Journal of pharmacology and experimental therapeutics.

[368]  C. Chavkin,et al.  Dynorphin is a specific endogenous ligand of the kappa opioid receptor. , 1982, Science.

[369]  M. Tyers A CLASSIFICATION OF OPIATE RECEPTORS THAT MEDIATE ANTINOCICEPTION IN ANIMALS , 1980, British journal of pharmacology.

[370]  L. Hood,et al.  Dynorphin-(1-13), an extraordinarily potent opioid peptide. , 1979, Proceedings of the National Academy of Sciences of the United States of America.

[371]  M. Nirenberg,et al.  Opiate-dependent modulation of adenylate cyclase. , 1977, Proceedings of the National Academy of Sciences of the United States of America.

[372]  John Hughes,et al.  Endogenous opioid peptides: multiple agonists and receptors , 1977, Nature.

[373]  A. Goldstein,et al.  Opioid activity of a peptide, beta-lipotropin-(61-91), derived from beta-lipotropin. , 1976, Proceedings of the National Academy of Sciences of the United States of America.

[374]  J. Thompson,et al.  The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog. , 1976, The Journal of pharmacology and experimental therapeutics.

[375]  H. Morris,et al.  Identification of two related pentapeptides from the brain with potent opiate agonist activity , 1975, Nature.

[376]  F. Leslie,et al.  EFFECT OF MORPHINE ON ADRENERGIC TRANSMISSION IN THE MOUSE VAS DEFERENS. ASSESSMENT OF AGONIST AND ANTAGONIST POTENCIES OF NARCOTIC ANALGESICS , 1975, British journal of pharmacology.

[377]  E. J. Simon,et al.  Stereospecific binding of the potent narcotic analgesic (3H) Etorphine to rat-brain homogenate. , 1973, Proceedings of the National Academy of Sciences of the United States of America.

[378]  S. Snyder,et al.  Opiate Receptor: Demonstration in Nervous Tissue , 1973, Science.

[379]  P. Portoghese A new concept on the mode of interaction of narcotic analgesics with receptors. , 1965, Journal of medicinal chemistry.

[380]  A H BECKETT,et al.  SYNTHETIC ANALGESICS: STEREOCHEMICAL CONSIDERATIONS , 1954, The Journal of pharmacy and pharmacology.

[381]  H. Kai,et al.  Discovery of naldemedine: A potent and orally available opioid receptor antagonist for treatment of opioid-induced adverse effects. , 2019, Bioorganic & medicinal chemistry letters.

[382]  R. Stevens,et al.  Structure of the human k-opioid receptor in complex with JDTic , 2012 .

[383]  J. Bidlack,et al.  Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. , 2009, Bioorganic & Medicinal Chemistry Letters.

[384]  M. Bruchas,et al.  Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase. , 2007, The Journal of biological chemistry.

[385]  J. Cassel,et al.  Amino acid conjugates as kappa opioid receptor agonists. , 2005, Bioorganic & medicinal chemistry letters.

[386]  David J. Daniels,et al.  Interaction of bivalent ligand KDN21 with heterodimeric delta-kappa opioid receptors in human embryonic kidney 293 cells. , 2005, Molecular pharmacology.

[387]  Y. Wong,et al.  Signal transducer and activator of transcription 3 activation by the delta-opioid receptor via Galpha14 involves multiple intermediates. , 2004, Molecular pharmacology.

[388]  J. Felger,et al.  Nociceptin/Orphanin FQ Increases Anxiety-Related Behavior and Circulating Levels of Corticosterone During Neophobic Tests of Anxiety , 2004, Neuropsychopharmacology.

[389]  E. Butelman,et al.  Effect of the endogenous kappa opioid agonist dynorphin A(1-17) on cocaine-evoked increases in striatal dopamine levels and cocaine-induced place preference in C57BL/6J mice. , 2004, Psychopharmacology.

[390]  Zhe Ding,et al.  kappa Opioid receptor interacts with Na(+)/H(+)-exchanger regulatory factor-1/Ezrin-radixin-moesin-binding phosphoprotein-50 (NHERF-1/EBP50) to stimulate Na(+)/H(+) exchange independent of G(i)/G(o) proteins. , 2004, The Journal of biological chemistry.

[391]  David J. Daniels,et al.  A bivalent ligand (KDN-21) reveals spinal delta and kappa opioid receptors are organized as heterodimers that give rise to delta(1) and kappa(2) phenotypes. Selective targeting of delta-kappa heterodimers. , 2004, Journal of medicinal chemistry.

[392]  U. Holzgrabe,et al.  Comparison of Pharmacological Activities of Three Distinct (cid:1) Ligands (Salvinorin A, TRK-820 and 3FLB) on (cid:1) Opioid Receptors in Vitro and Their Antipruritic and Antinociceptive Activities in Vivo , 2004 .

[393]  A. Beaudet,et al.  Regulation of delta-opioid receptor trafficking via mu-opioid receptor stimulation: evidence from mu-opioid receptor knock-out mice. , 2003, The Journal of neuroscience : the official journal of the Society for Neuroscience.

[394]  J. R. Palacio,et al.  The expression of delta- and kappa-opioid receptor is enhanced during intestinal inflammation in mice. , 2003, The Journal of pharmacology and experimental therapeutics.

[395]  N. Mello,et al.  Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors. , 2003, Journal of medicinal chemistry.

[396]  Angel Y. F. Kam,et al.  Rac and Cdc42-dependent regulation of c-Jun N-terminal kinases by the delta-opioid receptor. , 2003, Journal of neurochemistry.

[397]  Paul Ernsberger,et al.  Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist. , 2002, Proceedings of the National Academy of Sciences of the United States of America.

[398]  J. Kamei,et al.  Antipruritic activity of the kappa-opioid receptor agonist, TRK-820. , 2002, European journal of pharmacology.

[399]  D. Filliol,et al.  Motivational effects of cannabinoids are mediated by mu-opioid and kappa-opioid receptors. , 2002, The Journal of neuroscience : the official journal of the Society for Neuroscience.

[400]  P. Prather,et al.  Chronic agonist treatment converts antagonists into inverse agonists at delta-opioid receptors. , 2002, The Journal of pharmacology and experimental therapeutics.

[401]  R. Dannals,et al.  [(11)C]-GR89696, a potent kappa opiate receptor radioligand; in vivo binding of the R and S enantiomers. , 2002, Nuclear medicine and biology.

[402]  H. Nagase,et al.  Synthesis of optically active TAN-67, a highly selective delta opioid receptor agonist, and investigation of its pharmacological properties. , 2001, Drug design and discovery.

[403]  J. Pintar,et al.  Quantitative autoradiographic mapping of the ORL1, mu-, delta- and kappa-receptors in the brains of knockout mice lacking the ORL1 receptor gene. , 2001, Brain research.

[404]  J. Pintar,et al.  Expression of functional mu-opioid receptors during T cell development. , 2001, Journal of neuroimmunology.

[405]  D. Filliol,et al.  Autoradiographic mapping of the opioid receptor-like 1 (ORL1) receptor in the brains of mu-, delta- or kappa-opioid receptor knockout mice. , 2001, Neuroscience.

[406]  P. Singhal,et al.  Opiates promote T cell apoptosis through JNK and caspase pathway. , 2001, Advances in experimental medicine and biology.

[407]  A. Coop,et al.  BU48: a novel buprenorphine analog that exhibits delta-opioid-mediated convulsions but not delta-opioid-mediated antinociception in mice. , 2000, The Journal of pharmacology and experimental therapeutics.

[408]  P. Clarke,et al.  Antihyperalgesic effects of delta opioid agonists in a rat model of chronic inflammation. , 2000, British journal of pharmacology.

[409]  R. M. Jones,et al.  5'-Guanidinonaltrindole, a highly selective and potent kappa-opioid receptor antagonist. , 2000, European journal of pharmacology.

[410]  A. McKnight,et al.  Characterization of the ORL(1) receptor on adrenergic nerves in the rat anococcygeus muscle. , 2000, British journal of pharmacology.

[411]  H. Loh,et al.  Molecular mechanisms and regulation of opioid receptor signaling. , 2000, Annual review of pharmacology and toxicology.

[412]  C. Mandyam,et al.  beta-Funaltrexamine inactivates ORL1 receptors in BE(2)-C human neuroblastoma cells. , 2000, European journal of pharmacology.

[413]  A. Dierich,et al.  Mice deficient for delta- and mu-opioid receptors exhibit opposing alterations of emotional responses. , 2000, Nature genetics.

[414]  H. Akil,et al.  Constitutive activity of the delta-opioid receptor expressed in C6 glioma cells: identification of non-peptide delta-inverse agonists. , 1999, British journal of pharmacology.

[415]  A. Ho,et al.  Dynorphin A1-13 causes elevation of serum levels of prolactin through an opioid receptor mechanism in humans: gender differences and implications for modulation of dopaminergic tone in the treatment of addictions. , 1999, The Journal of pharmacology and experimental therapeutics.

[416]  U. Scheffel,et al.  Selective in vivo binding of [3H]naltriben to delta-opioid receptors in mouse brain. , 1998, European journal of pharmacology.

[417]  Y. Wong,et al.  Differential coupling of mu-, delta-, and kappa-opioid receptors to G alpha16-mediated stimulation of phospholipase C. , 1998, Journal of neurochemistry.

[418]  V. Ganapathy,et al.  Cloning and functional characterization of a sigma receptor from rat brain. , 1998, Journal of neurochemistry.

[419]  A. Kastin,et al.  A potent and selective endogenous agonist for the mu-opiate receptor. , 1997, Nature.

[420]  R. Quock,et al.  Relative efficacies of delta-opioid receptor agonists at the cloned human delta-opioid receptor. , 1997, European journal of pharmacology.

[421]  H. Matthes,et al.  Quantitative autoradiographic mapping of mu-, delta- and kappa-opioid receptors in knockout mice lacking the mu-opioid receptor gene. , 1997, Brain research.

[422]  L. Liu-Chen,et al.  Dual ultrastructural immunocytochemical labeling of mu and delta opioid receptors in the superficial layers of the rat cervical spinal cord. , 1997, Brain research.

[423]  K. Fukuda,et al.  Functional coupling of the delta-, mu-, and kappa-opioid receptors to mitogen-activated protein kinase and arachidonate release in Chinese hamster ovary cells. , 1996, Journal of neurochemistry.

[424]  D. Grandy,et al.  Functional antagonism of mu-, delta- and kappa-opioid antinociception by orphanin FQ. , 1996, Neuroscience letters.

[425]  S. Childers,et al.  Identification of opioid receptor-like (ORL1) peptide-stimulated [35S]GTP gamma S binding in rat brain. , 1996, Neuroreport.

[426]  E. J. Simon,et al.  Autoradiographic comparison of [3H]DPDPE and [3H]DSLET binding: evidence for distinct delta 1 and delta 2 opioid receptor populations in rat brain. , 1996, Brain research.

[427]  V. Pickel,et al.  mu Opiate receptor immunoreactivity in rat central nervous system. , 1996, Neurochemical research.

[428]  K. Mackie,et al.  Modulation of Ca2+ channels by G-protein beta gamma subunits. , 1996, Nature.

[429]  H. Loh,et al.  Cloning and promoter mapping of mouse kappa opioid receptor gene. , 1995, Biochemical and biophysical research communications.

[430]  F. Simonin,et al.  Identification of kappa- and delta-opioid receptor transcripts in immune cells. , 1995, FEBS letters.

[431]  Y. Wong,et al.  Gz coupling to the rat kappa-opioid receptor. , 1995, FEBS letters.

[432]  C. Chen,et al.  Cloning of a human kappa opioid receptor from the brain. , 1995, Life sciences.

[433]  T. Eisenstein,et al.  Sequence of kappa-opioid receptor cDNA in the R1.1 thymoma cell line. , 1995, Journal of neuroimmunology.

[434]  H. Ueda,et al.  Opioid mu- and kappa-receptor mediate phospholipase C activation through Gi1 in Xenopus oocytes. , 1995, Brain research. Molecular brain research.

[435]  K. Fukuda,et al.  Coupling of the cloned mu-opioid receptor with the omega-conotoxin-sensitive Ca2+ current in NG108-15 cells. , 1995, Journal of neurochemistry.

[436]  M. Mortrud,et al.  Molecular cloning and tissue distribution of a putative member of the rat opioid receptor gene family that is not a mu, delta or kappa opioid receptor type. , 1994, FEBS letters.

[437]  D. Yang,et al.  Isolation of a human kappa opioid receptor cDNA from placenta. , 1994, Biochemical and biophysical research communications.

[438]  B. O'dowd,et al.  Cloning, characterization, and distribution of a mu-opioid receptor in rat brain. , 1994, Journal of neurochemistry.

[439]  M. Satoh,et al.  Molecular cloning and in situ hybridization histochemistry for rat mu-opioid receptor. , 1994, Neuroscience research.

[440]  R J Knapp,et al.  Identification of a human delta opioid receptor: cloning and expression. , 1994, Life sciences.

[441]  C. Kozak,et al.  Murine chromosomal location of the mu and kappa opioid receptor genes. , 1994, Genomics.

[442]  S. Kaneko,et al.  Cloning and expression of a cDNA for the rat kappa-opioid receptor. , 1993, FEBS letters.

[443]  K. Mori,et al.  Primary structures and expression from cDNAs of rat opioid receptor delta- and mu-subtypes. , 1993, FEBS letters.

[444]  F. Porreca,et al.  Lack of cross-tolerance between U69,593 and bremazocine suggests kappa-opioid receptor multiplicity in mice. , 1993, European journal of pharmacology.

[445]  G H Loew,et al.  Molecular determinants of mu receptor recognition for the fentanyl class of compounds. , 1992, Molecular pharmacology.

[446]  M. Adler,et al.  Effect of mu-, kappa-, and delta-selective opioid agonists on thermoregulation in the rat. , 1992, Pharmacology, biochemistry, and behavior.

[447]  A. Borsodi,et al.  Synthesis and binding characteristics of the highly delta-specific new tritiated opioid peptide, [3H]deltorphin II. , 1992, Life sciences.

[448]  T. Nakazawa,et al.  Spinal kappa receptor-mediated analgesia of E-2078, a systemically active dynorphin analog, in mice. , 1991, The Journal of pharmacology and experimental therapeutics.

[449]  I. Zagon,et al.  Zeta (zeta), a growth-related opioid receptor in developing rat cerebellum: identification and characterization. , 1991, Brain research.

[450]  D. Besse,et al.  Autoradiographic distribution of mu, delta and kappa opioid binding sites in the superficial dorsal horn, over the rostrocaudal axis of the rat spinal cord. , 1991, Brain Research.

[451]  R. Zukin,et al.  Neuroanatomical localization of kappa 1 and kappa 2 opioid receptors in rat and guinea pig brain. , 1991, Brain research.

[452]  H. Yoshino,et al.  Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogues. , 1990, Journal of medicinal chemistry.

[453]  J. Besson,et al.  Pre- and postsynaptic distribution of mu, delta and kappa opioid receptors in the superficial layers of the cervical dorsal horn of the rat spinal cord. , 1990, Brain research.

[454]  K. Rice,et al.  Pharmacological activities of optically pure enantiomers of the kappa opioid agonist, U50,488, and its cis diastereomer: evidence for three kappa receptor subtypes. , 1989, European journal of pharmacology.

[455]  C. Smith,et al.  Opioid receptors in the mouse ileum. , 1988, Archives internationales de pharmacodynamie et de therapie.

[456]  K. Rice,et al.  Mu-, delta- and kappa-opioid receptor-mediated inhibition of neurotransmitter release and adenylate cyclase activity in rat brain slices: studies with fentanyl isothiocyanate. , 1988, European journal of pharmacology.

[457]  T. Cicero,et al.  Autoradiography of [3H]U-69593 binding sites in rat brain: evidence for kappa opioid receptor subtypes. , 1988, European journal of pharmacology.

[458]  P. Portoghese,et al.  Naltrindole, a highly selective and potent non-peptide delta opioid receptor antagonist. , 1988, European journal of pharmacology.

[459]  M. Yeadon,et al.  Comparative binding of mu and delta selective ligands in whole brain and pons/medulla homogenates from rat: affinity profiles of fentanyl derivatives. , 1988, Neuropharmacology.

[460]  V. Hruby,et al.  Quantitative autoradiography of [3H]CTOP binding to mu opioid receptors in rat brain. , 1988, Life sciences.

[461]  M. Adler,et al.  Hypothermia and poikilothermia induced by a kappa-agonist opioid and a neuroleptic. , 1987, European journal of pharmacology.

[462]  T. Shippenberg,et al.  Place preference conditioning reveals the involvement of D1-dopamine receptors in the motivational properties of mu- and kappa-opioid agonists. , 1987, Brain research.

[463]  B. Attali,et al.  Inhibition of adenylate cyclase and induction of heterologous desensitization by kappa agonists in rat spinal cord. , 1986, NIDA research monograph.

[464]  L. Krulich,et al.  Opioid kappa receptors and the secretion of prolactin (PRL) and growth hormone (GH) in the rat. II. GH and PRL release-inhibiting effects of the opioid kappa receptor agonists bremazocine and U-50,488. , 1986, Neuroendocrinology.

[465]  K. Mann,et al.  Anterior pituitary hormone responses to a kappa-opioid agonist in man. , 1986, The Journal of clinical endocrinology and metabolism.

[466]  V. Hruby,et al.  Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors. , 1986, Journal of medicinal chemistry.

[467]  J. Morley,et al.  The kappa opioid receptor and food intake. , 1985, European journal of pharmacology.

[468]  J. Mccall,et al.  [3H]U-69593 a highly selective ligand for the opioid kappa receptor. , 1985, European journal of pharmacology.

[469]  W. Sadee,et al.  Characterization of a labile naloxone binding site (lambda site) in rat brain. , 1985, Journal of neurochemistry.

[470]  T. Yaksh,et al.  The physiology and pharmacology of spinal opiates. , 1985, Annual review of pharmacology and toxicology.

[471]  T. Yaksh,et al.  In vivo studies on spinal opiate receptor systems mediating antinociception. II. Pharmacological profiles suggesting a differential association of mu, delta and kappa receptors with visceral chemical and cutaneous thermal stimuli in the rat. , 1984, The Journal of pharmacology and experimental therapeutics.

[472]  C. Chavkin,et al.  Comparison of dynorphin-selective Kappa receptors in mouse vas deferens and guinea pig ileum. Spare receptor fraction as a determinant of potency. , 1983, Molecular pharmacology.

[473]  R. Lahti,et al.  U-50,488: a selective and structurally novel non-Mu (kappa) opioid agonist. , 1983, The Journal of pharmacology and experimental therapeutics.

[474]  B. Morgan,et al.  Analogues of beta-LPH61-64 possessing selective agonist activity at mu-opiate receptors. , 1981, European journal of pharmacology.

[475]  R. Schulz,et al.  Specificity of opioids towards the mu-, delta- and epsilon-opiate receptors. , 1979, Neuroscience letters.