Reversal of subtype-selectivity and function by the introduction of a para-benzamidyl substituent to N-cyclopropylmethyl nornepenthone.
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Wei-Chang Fu | Wei Li | Qiong Xie | Liming Shao | Yu-Jun Wang | X. Liu | Rongrong Ye | Linghui Kong | Zixiang Li | Jinggen Liu | Yun Fang | Jing-rui Chai | Baiyu Chen | Kuan Ning | Jiashuo Lu | Shuang Jiang | Siyuan Tang | Yingjie Lan | Xiaobo Mai | Jing‐rui Chai
[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] Wei-Chang Fu,et al. SLL-627 Is a Highly Selective and Potent κ Opioid Receptor (KOR) Agonist with an Unexpected Nonreduction in Locomotor Activity. , 2022, Journal of medicinal chemistry.
[5] G. Skiniotis,et al. Structure‐Based Evolution of G Protein‐Biased μ‐Opioid Receptor Agonists , 2022, bioRxiv.
[6] B. Armoon,et al. Mental health status, health service utilization, drug use behaviors associated with non-fatal overdose among people who use illicit drugs: A meta-analysis , 2021, Journal of Substance Use.
[7] Joseph M. Paggi,et al. Insights into distinct signaling profiles of the µOR activated by diverse agonists , 2022, Nature Chemical Biology.
[8] M. Karamouzian,et al. Mental disorder and opioid overdose: a systematic review , 2021, Social Psychiatry and Psychiatric Epidemiology.
[9] M. J. Robertson,et al. Structure Determination of Inactive-State GPCRs with a Universal Nanobody , 2021, bioRxiv.
[10] Wei-Chang Fu,et al. Discovery of an M-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethanotetrahydronorthebaine as a Selective, Potent, and Orally Active κ-Opioid Receptor Agonist with an Improved Central Nervous System Safety Profile. , 2021, Journal of medicinal chemistry.
[11] Wei-Chang Fu,et al. Discovery, Structure-Activity Relationship, and Mechanistic Studies of 1-((3R,4S)-3-((Dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)piperidin-1-yl)-2-(2,4,5-trifluorophenyl)ethan-1-one as a Novel Potent Analgesic. , 2021, Journal of Medicinal Chemistry.
[12] R. M. Krausz,et al. The opioid overdose crisis as a global health challenge , 2021, Current opinion in psychiatry.
[13] M. Manzar,et al. Emerging Challenges in COVID-19 With Substance Use Disorders , 2021, Addictive Disorders & Their Treatment.
[14] L. Manchikanti,et al. COVID-19 and the Opioid Epidemic: Two Public Health Emergencies That Intersect With Chronic Pain , 2021, Pain and Therapy.
[15] S. Shoptaw,et al. The opioid crisis and HIV in the USA: deadly synergies , 2021, The Lancet.
[16] Yan Zhang,et al. Computational insights into the molecular mechanisms of differentiated allosteric modulation at the mu opioid receptor by structurally similar bitopic modulators , 2020, Journal of Computer-Aided Molecular Design.
[17] N. Volkow,et al. The Changing Opioid Crisis: development, challenges and opportunities , 2020, Molecular Psychiatry.
[18] J. Bell,et al. Medication Treatment of Opioid Use Disorder , 2020, Biological Psychiatry.
[19] D. Selley,et al. Application of Bivalent Bioisostere Concept on Design and Discovery of Potent Opioid Receptor Modulators. , 2019, Journal of medicinal chemistry.
[20] Wei Li,et al. Discovery of a highly selective and potent kappa opioid receptor agonist from N-cyclopropylmethyl-7α-phenyl-6,14-endoethano-tetrahydro- northebaines with reduced central nervous system (CNS) side effects navigated by the message-address concept. , 2019, Journal of medicinal chemistry.
[21] R. Stevens,et al. Elucidating the active δ-opioid receptor crystal structure with peptide and small-molecule agonists , 2019, Science Advances.
[22] S. Naveed,et al. A Review of Samidorphan: A Novel Opioid Antagonist , 2019, Cureus.
[23] N. Volkow,et al. Prevention and Treatment of Opioid Misuse and Addiction: A Review , 2019, JAMA psychiatry.
[24] 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.
[25] D. Selley,et al. Structure-Activity Relationship Studies of 6α- and 6β-Indolylacetamidonaltrexamine Derivatives as Bitopic Mu Opioid Receptor Modulators and Elaboration of the "Message-Address Concept" To Comprehend Their Functional Conversion. , 2018, ACS chemical neuroscience.
[26] G. Walker. The opioid crisis: a 21st century pain. , 2018, Drugs of today.
[27] Ryan T. Strachan,et al. Structure of the Nanobody-Stabilized Active State of the Kappa Opioid Receptor , 2018, Cell.
[28] Wei-Chang Fu,et al. The Pharmacological Heterogeneity of Nepenthone Analogs in Conferring Highly Selective and Potent κ-Opioid Agonistic Activities. , 2017, ACS chemical neuroscience.
[29] Stephen M. Husbands,et al. Structural insights into μ-opioid receptor activation , 2015, Nature.
[30] G. Kellogg,et al. Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands. , 2015, Bioorganic & medicinal chemistry.
[31] E. Bullmore,et al. The opioid receptor pharmacology of GSK1521498 compared to other ligands with differential effects on compulsive reward-related behaviours , 2014, Psychopharmacology.
[32] D. Selley,et al. Design, synthesis, and biological evaluation of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4'-pyridyl)carboxamido]morphinan derivatives as peripheral selective μ opioid receptor Agents. , 2012, Journal of medicinal chemistry.
[33] Aashish Manglik,et al. Structure of the δ-opioid receptor bound to naltrindole , 2012, Nature.
[34] L. Pardo,et al. Crystal structure of the μ-opioid receptor bound to a morphinan antagonist , 2012, Nature.
[35] Bryan L. Roth,et al. Structure of the human kappa opioid receptor in complex with JDTic , 2012, Nature.
[36] Yun Tang,et al. Synthesis and evaluation of κ-opioid receptor agonistic activity and antinociceptive effect of novel morphine analogues, 7α-phenyl-6α,14α-endo-etheno-tetrahydrothebaine with substituted o-, m- and p-amino group , 2011, Medicinal Chemistry Research.
[37] K. Rice,et al. Identification of a novel “almost neutral” μ‐opioid receptor antagonist in CHO cells expressing the cloned human μ‐opioid receptor , 2010, Synapse.
[38] D. Selley,et al. Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists. , 2009, Journal of medicinal chemistry.
[39] Y. Long,et al. LPK-26, a novel kappa-opioid receptor agonist with potent antinociceptive effects and low dependence potential. , 2008, European journal of pharmacology.
[40] W. Schmidt,et al. Alvimopan* (ADL 8-2698) is a novel peripheral opioid antagonist. , 2001, American journal of surgery.
[41] D. Ferguson,et al. Transformation of a κ-Opioid Receptor Antagonist to a κ-Agonist by Transfer of a Guanidinium Group from the 5‘- to 6‘-Position of Naltrindole , 2001 .
[42] T. Sumpter,et al. Methocinnamox is a potent, long-lasting, and selective antagonist of morphine-mediated antinociception in the mouse: comparison with clocinnamox, beta-funaltrexamine, and beta-chlornaltrexamine. , 2000, The Journal of pharmacology and experimental therapeutics.
[43] P. Portoghese,et al. 5'-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist , 2000 .
[44] B. Roques,et al. μ-Opioid receptor specific antagonist cyprodime: characterization by in vitro radioligand and [35S]GTPγS binding assays , 1999 .
[45] H. Nagase,et al. Pharmacological properties of TRK-820 on cloned μ-, δ- and κ-opioid receptors and nociceptin receptor , 1999 .
[46] J. Woods,et al. Clocinnamox: a novel, systemically-active, irreversible opioid antagonist. , 1992, The Journal of pharmacology and experimental therapeutics.
[47] P. Portoghese,et al. Design of peptidomimetic delta opioid receptor antagonists using the message-address concept. , 1990, Journal of medicinal chemistry.
[48] Kunjea Kim,et al. Synthesis of the New Thebaine Derivatives by the Diels-Alder Reaction with Northebaine , 1989 .
[49] J. P. Gonzalez,et al. Naltrexone , 1988, Drugs.
[50] P. Portoghese,et al. Application of the message-address concept in the design of highly potent and selective non-peptide delta opioid receptor antagonists. , 1988, Journal of medicinal chemistry.
[51] D. Weidler,et al. Nalmefene: Safety and Kinetics After Single and Multiple Oral Doses of a New Opioid Antagonist , 1987, Journal of clinical pharmacology.
[52] T. Gal,et al. Prolonged blockade of opioid effect with oral nalmefene , 1986, Clinical pharmacology and therapeutics.
[53] D. L. Larson,et al. Opioid receptor binding characteristics of the non-equilibrium μ antagonist, β-funaltrexamine (β-FNA)☆ , 1985 .
[54] D. Sessler,et al. Opioid-Induced Bowel Dysfunction , 2012, Drugs.
[55] Yun Tang,et al. Highly selective and potent mu opioid ligands by unexpected substituent on morphine skeleton. , 2010, Bioorganic & medicinal chemistry letters.
[56] P. M. Goodrich. Naloxone hydrochloride: a review. , 1990, AANA journal.