Pharmacology of metabotropic glutamate receptor allosteric modulators: structural basis and therapeutic potential for CNS disorders.

[1]  Yuko Fujita,et al.  Therapeutic effects of metabotropic glutamate receptor 5 positive allosteric modulator CDPPB on phencyclidine‐induced cognitive deficits in mice , 2013, Fundamental & clinical pharmacology.

[2]  A. Sławinska,et al.  Anxiolytic- but not antidepressant-like activity of Lu AF21934, a novel, selective positive allosteric modulator of the mGlu4 receptor , 2013, Neuropharmacology.

[3]  G. Marek,et al.  CNS distribution of metabotropic glutamate 2 and 3 receptors: Transgenic mice and [3H]LY459477 autoradiography , 2013, Neuropharmacology.

[4]  T. Wichmann,et al.  Metabotropic glutamate receptor 4 in the basal ganglia of parkinsonian monkeys: Ultrastructural localization and electrophysiological effects of activation in the striatopallidal complex , 2013, Neuropharmacology.

[5]  P. Conn,et al.  Functional selectivity induced by mGlu4 receptor positive allosteric modulation and concomitant activation of Gq coupled receptors , 2013, Neuropharmacology.

[6]  Kari A. Johnson,et al.  The metabotropic glutamate receptor 8 agonist (S)-3,4-DCPG reverses motor deficits in prolonged but not acute models of Parkinson's disease , 2013, Neuropharmacology.

[7]  P. Gubellini,et al.  Synergy between l-DOPA and a novel positive allosteric modulator of metabotropic glutamate receptor 4: Implications for Parkinson's disease treatment and dyskinesia , 2013, Neuropharmacology.

[8]  E. Sher,et al.  Pharmacological profiling of native group II metabotropic glutamate receptors in primary cortical neuronal cultures using a FLIPR , 2013, Neuropharmacology.

[9]  J. Brennan,et al.  Negative allosteric modulation of metabotropic glutamate receptor 5 results in broad spectrum activity relevant to treatment resistant depression , 2013, Neuropharmacology.

[10]  M. Olive,et al.  Attenuation of methamphetamine seeking by the mGluR2/3 agonist LY379268 in rats with histories of restricted and escalated self-administration , 2013, Neuropharmacology.

[11]  S. Chaki,et al.  mGlu2/3 and mGlu5 receptors: Potential targets for novel antidepressants , 2013, Neuropharmacology.

[12]  Lei Shi,et al.  Molecular determinants of selectivity and efficacy at the dopamine D3 receptor. , 2012, Journal of medicinal chemistry.

[13]  M. Betts,et al.  Allosteric modulation of the group III mGlu4 receptor provides functional neuroprotection in the 6‐hydroxydopamine rat model of Parkinson's disease , 2012, British journal of pharmacology.

[14]  Eric J Miller,et al.  Ligand Bias at Metabotropic Glutamate 1a Receptors: Molecular Determinants That Distinguish β-Arrestin-Mediated from G Protein-Mediated Signaling , 2012, Molecular Pharmacology.

[15]  Cody J. Wenthur,et al.  Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM. , 2012, Bioorganic & medicinal chemistry letters.

[16]  Brian A. Chauder,et al.  Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor. , 2012, Bioorganic & medicinal chemistry letters.

[17]  D. Doller,et al.  4-(1-Phenyl-1H-pyrazol-4-yl)quinolines as novel, selective and brain penetrant metabotropic glutamate receptor 4 positive allosteric modulators. , 2012, Bioorganic & medicinal chemistry letters.

[18]  M. Olive,et al.  Metabotropic glutamate receptors and drug addiction , 2012 .

[19]  T. Frimurer,et al.  Reversed binding of a small molecule ligand in homologous chemokine receptors – differential role of extracellular loop 2 , 2012, British journal of pharmacology.

[20]  Jacqueline N. Crawley,et al.  Negative Allosteric Modulation of the mGluR5 Receptor Reduces Repetitive Behaviors and Rescues Social Deficits in Mouse Models of Autism , 2012, Science Translational Medicine.

[21]  A. Bahi The selective metabotropic glutamate receptor 7 allosteric agonist AMN082 prevents reinstatement of extinguished ethanol-induced conditioned place preference in mice , 2012, Pharmacology Biochemistry and Behavior.

[22]  M. Amalric,et al.  Antiparkinsonian action of a selective group III mGlu receptor agonist is associated with reversal of subthalamonigral overactivity , 2012, Neurobiology of Disease.

[23]  H. Daniel,et al.  A novel selective metabotropic glutamate receptor 4 agonist reveals new possibilities for developing subtype selective ligands with therapeutic potential , 2012, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

[24]  M. Bear,et al.  Chronic Pharmacological mGlu5 Inhibition Corrects Fragile X in Adult Mice , 2012, Neuron.

[25]  M. Fendt,et al.  Pharmacological interference with metabotropic glutamate receptor subtype 7 but not subtype 5 differentially affects within- and between-session extinction of Pavlovian conditioned fear , 2012, Neuropharmacology.

[26]  E. Klann,et al.  Metabotropic glutamate receptor-dependent long-term depression is impaired due to elevated ERK signaling in the ΔRG mouse model of tuberous sclerosis complex , 2012, Neurobiology of Disease.

[27]  F. Gasparini,et al.  Pharmacological modulation of mGluR7 with AMN082 and MMPIP exerts specific influences on alcohol consumption and preference in rats , 2012, Addiction biology.

[28]  Esther Kellenberger,et al.  Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors. , 2012, Journal of medicinal chemistry.

[29]  W. Greenlee,et al.  Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain. , 2012, Bioorganic & medicinal chemistry letters.

[30]  S. Duty,et al.  Antiparkinsonian potential of targeting group III metabotropic glutamate receptor subtypes in the rodent substantia nigra pars reticulata , 2012, British journal of pharmacology.

[31]  H. Lavreysen,et al.  Functional Impact of Allosteric Agonist Activity of Selective Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 in Regulating Central Nervous System Function , 2012, Molecular Pharmacology.

[32]  Anna L. Blobaum,et al.  The Metabotropic Glutamate Receptor 4-Positive Allosteric Modulator VU0364770 Produces Efficacy Alone and in Combination with l-DOPA or an Adenosine 2A Antagonist in Preclinical Rodent Models of Parkinson's Disease , 2012, Journal of Pharmacology and Experimental Therapeutics.

[33]  Manfred Schneider,et al.  Characterization of an mGluR2/3 Negative Allosteric Modulator in Rodent Models of Depression , 2011, Journal of neurogenetics.

[34]  Anna L. Blobaum,et al.  Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkins , 2011, Journal of medicinal chemistry.

[35]  Mark F. Bear,et al.  Mutations causing syndromic autism define an axis of synaptic pathophysiology , 2011, Nature.

[36]  C. Bissantz,et al.  Structural determinants of allosteric antagonism at metabotropic glutamate receptor 2: mechanistic studies with new potent negative allosteric modulators , 2011, British journal of pharmacology.

[37]  J. Os,et al.  The size and burden of mental disorders and other disorders of the brain in Europe 2010 , 2011, European Neuropsychopharmacology.

[38]  S. Dolan,et al.  Activation of metabotropic glutamate receptor 7 in spinal cord inhibits pain and hyperalgesia in a novel formalin model in sheep , 2011, Behavioural pharmacology.

[39]  G. Labesse,et al.  Interdomain movements in metabotropic glutamate receptor activation , 2011, Proceedings of the National Academy of Sciences.

[40]  S. Stauffer,et al.  Progress toward positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5). , 2011, ACS chemical neuroscience.

[41]  A. Robichaud,et al.  Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators. , 2011, Journal of medicinal chemistry.

[42]  J. Dwyer,et al.  The Metabotropic Glutamate Receptor 7 Allosteric Modulator AMN082: A Monoaminergic Agent in Disguise? , 2011, Journal of Pharmacology and Experimental Therapeutics.

[43]  I. Liberzon,et al.  The Neurocircuitry of Fear, Stress, and Anxiety Disorders , 2011, Neuropsychopharmacology.

[44]  B. Kinon,et al.  A Multicenter, Inpatient, Phase 2, Double-Blind, Placebo-Controlled Dose-Ranging Study of LY2140023 Monohydrate in Patients With DSM-IV Schizophrenia , 2011, Journal of clinical psychopharmacology.

[45]  F. Nicoletti,et al.  Metabotropic glutamate receptors: From the workbench to the bedside , 2011, Neuropharmacology.

[46]  Jeffrey S. Smith,et al.  Preclinical profile of a novel metabotropic glutamate receptor 5 positive allosteric modulator. , 2011, European journal of pharmacology.

[47]  C. Lindsley,et al.  Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists. , 2011, Bioorganic & medicinal chemistry letters.

[48]  C. Langmead,et al.  Quantitative Analysis Reveals Multiple Mechanisms of Allosteric Modulation of the mGlu5 Receptor in Rat Astroglia , 2011, Molecular Pharmacology.

[49]  P Jeffrey Conn,et al.  "Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology. , 2011, Biochemistry.

[50]  M. Sahin,et al.  Mechanisms of neurocognitive dysfunction and therapeutic considerations in tuberous sclerosis complex. , 2011, Current opinion in neurology.

[51]  E. Nisenbaum,et al.  Targeting Group II Metabotropic Glutamate (mGlu) Receptors for the Treatment of Psychosis Associated with Alzheimer's Disease: Selective Activation of mGlu2 Receptors Amplifies β-Amyloid Toxicity in Cultured Neurons, Whereas Dual Activation of mGlu2 and mGlu3 Receptors Is Neuroprotective , 2011, Molecular Pharmacology.

[52]  J. Shumsky,et al.  Group II Metabotropic Glutamate Receptor Agonist Ameliorates MK801-Induced Dysfunction of NMDA Receptors via the Akt/GSK-3β Pathway in Adult Rat Prefrontal Cortex , 2011, Neuropsychopharmacology.

[53]  Jens Meiler,et al.  Allosteric modulation of metabotropic glutamate receptors: Structural insights and therapeutic potential , 2011, Neuropharmacology.

[54]  D. Sheffler,et al.  Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats. , 2011, Journal of medicinal chemistry.

[55]  G. Marek,et al.  N-(4-((2-(trifluoromethyl)-3-hydroxy-4-(isobutyryl)phenoxy)methyl)benzyl)-1-methyl-1H-imidazole-4-carboxamide (THIIC), a Novel Metabotropic Glutamate 2 Potentiator with Potential Anxiolytic/Antidepressant Properties: In Vivo Profiling Suggests a Link between Behavioral and Central Nervous System Neu , 2011, Journal of Pharmacology and Experimental Therapeutics.

[56]  H. Schoemaker,et al.  Effects of a Positive Allosteric Modulator of Group II Metabotropic Glutamate Receptors, LY487379, on Cognitive Flexibility and Impulsive-Like Responding in Rats , 2010, Journal of Pharmacology and Experimental Therapeutics.

[57]  P Jeffrey Conn,et al.  Discovery of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Reveals Chemical and Functional Diversity and In Vivo Activity in Rat Behavioral Models of Anxiolytic and Antipsychotic Activity , 2010, Molecular Pharmacology.

[58]  S. Schann,et al.  Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators. , 2010, Journal of medicinal chemistry.

[59]  S. Jadhav,et al.  Discovery of N-Aryl Piperazines as Selective mGluR5 Potentiators with Improved In Vivo Utility , 2010 .

[60]  K. Myers,et al.  Extinction of drug- and withdrawal-paired cues in animal models: Relevance to the treatment of addiction , 2010, Neuroscience & Biobehavioral Reviews.

[61]  Andrzej Pilc,et al.  The Antidepressant-Like Action of Metabotropic Glutamate 7 Receptor Agonist N,N′-Bis(Diphenylmethyl)-1,2-Ethanediamine (AMN082) Is Serotonin-Dependent , 2010, Journal of Pharmacology and Experimental Therapeutics.

[62]  Z. Xi,et al.  Activation of mGluR7s inhibits cocaine‐induced reinstatement of drug‐seeking behavior by a nucleus accumbens glutamate‐mGluR2/3 mechanism in rats , 2010, Journal of neurochemistry.

[63]  Qin Li,et al.  A mGluR5 antagonist under clinical development improves L-DOPA-induced dyskinesia in parkinsonian rats and monkeys , 2010, Neurobiology of Disease.

[64]  K. Gregory,et al.  Discovery of a Novel Chemical Class of mGlu5 Allosteric Ligands with Distinct Modes of Pharmacology , 2010, ACS chemical neuroscience.

[65]  S. Ametamey,et al.  Syntheses and pharmacological characterization of novel thiazole derivatives as potential mGluR5 PET ligands. , 2010, Bioorganic & Medicinal Chemistry.

[66]  S. Okuda,et al.  Effects of a novel metabotropic glutamate receptor 7 negative allosteric modulator, 6-(4-methoxyphenyl)-5-methyl-3-pyridin-4-ylisoxazonolo[4,5-c]pyridin-4(5H)-one (MMPIP), on the central nervous system in rodents. , 2010, European journal of pharmacology.

[67]  A. Stuchlik,et al.  The difference in effect of mGlu2/3 and mGlu5 receptor agonists on cognitive impairment induced by MK-801. , 2010, European journal of pharmacology.

[68]  B. Moghaddam,et al.  Activation of type 5 metabotropic glutamate receptors attenuates deficits in cognitive flexibility induced by NMDA receptor blockade. , 2010, European journal of pharmacology.

[69]  F. Zerbib,et al.  Efficacy, tolerability and pharmacokinetics of a modified release formulation of ADX10059, a negative allosteric modulator of metabotropic glutamate receptor 5: an esophageal pH‐impedance study in healthy subjects , 2010, Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society.

[70]  S. Bicciato,et al.  Metabotropic glutamate receptor-4 modulates adaptive immunity and restrains neuroinflammation , 2010, Nature Medicine.

[71]  F. Weiss,et al.  Behavioral and Functional Evidence of Metabotropic Glutamate Receptor 2/3 and Metabotropic Glutamate Receptor 5 Dysregulation in Cocaine-Escalated Rats: Factor in the Transition to Dependence , 2010, Biological Psychiatry.

[72]  J. Kim,et al.  Impaired Extinction Retention in Adolescent Rats: Effects of D-Cycloserine , 2010, Neuropsychopharmacology.

[73]  D. Sheffler,et al.  The mGluR2 Positive Allosteric Modulator BINA Decreases Cocaine Self-Administration and Cue-Induced Cocaine-Seeking and Counteracts Cocaine-Induced Enhancement of Brain Reward Function in Rats , 2010, Neuropsychopharmacology.

[74]  J. Gore,et al.  Selective potentiation of the metabotropic glutamate receptor subtype 2 blocks phencyclidine-induced hyperlocomotion and brain activation , 2010, Neuroscience.

[75]  F. Weiss,et al.  Effects of the mGlu2/3 Agonist LY379268 and the mGlu5 Antagonist MTEP on Ethanol Seeking and Reinforcement Are Differentially Altered in Rats with a History of Ethanol Dependence , 2010, Biological Psychiatry.

[76]  Sarah L. Huszar,et al.  MK-801 produces a deficit in sucrose preference that is reversed by clozapine, d-serine, and the metabotropic glutamate 5 receptor positive allosteric modulator CDPPB: Relevance to negative symptoms associated with schizophrenia? , 2010, Pharmacology Biochemistry and Behavior.

[77]  M. Amalric,et al.  Metabotropic Glutamate 7 Receptor Subtype Modulates Motor Symptoms in Rodent Models of Parkinson's Disease , 2010, Journal of Pharmacology and Experimental Therapeutics.

[78]  Kari A. Johnson,et al.  Context-Dependent Pharmacology Exhibited by Negative Allosteric Modulators of Metabotropic Glutamate Receptor 7 , 2010, Molecular Pharmacology.

[79]  Younglim Lee,et al.  Glutamatergic (N-Methyl-d-aspartate Receptor) Hypofrontality in Schizophrenia: Too Little Juice or a Miswired Brain? , 2010, Molecular Pharmacology.

[80]  W. Danysz,et al.  Effects of a positive allosteric modulator of mGluR5 ADX47273 on conditioned avoidance response and PCP-induced hyperlocomotion in the rat as models for schizophrenia , 2010, Pharmacology Biochemistry and Behavior.

[81]  K. Gerlach,et al.  mGluR4 positive allosteric modulators with potential for the treatment of Parkinson's disease: WO09010455 , 2010, Expert opinion on therapeutic patents.

[82]  Maiken Nedergaard,et al.  Glial calcium and diseases of the nervous system. , 2010, Cell calcium.

[83]  P. Conn,et al.  Metabotropic glutamate receptors: physiology, pharmacology, and disease. , 2010, Annual review of pharmacology and toxicology.

[84]  R A John Challiss,et al.  Effects of Positive Allosteric Modulators on Single-Cell Oscillatory Ca2+ Signaling Initiated by the Type 5 Metabotropic Glutamate Receptor , 2009, Molecular Pharmacology.

[85]  P Jeffrey Conn,et al.  Glutamate receptors as therapeutic targets for Parkinson's disease. , 2009, CNS & neurological disorders drug targets.

[86]  W. Danysz,et al.  Comparison of the mGlu(5) receptor positive allosteric modulator ADX47273 and the mGlu(2/3) receptor agonist LY354740 in tests for antipsychotic-like activity. , 2009, European journal of pharmacology.

[87]  M. Quirk,et al.  A Selective Allosteric Potentiator of the M1 Muscarinic Acetylcholine Receptor Increases Activity of Medial Prefrontal Cortical Neurons and Restores Impairments in Reversal Learning , 2009, The Journal of Neuroscience.

[88]  F. Aboitiz,et al.  Molecular mechanisms underlying glutamatergic dysfunction in schizophrenia: therapeutic implications , 2009, Journal of neurochemistry.

[89]  A. Volterra,et al.  Astrocytic dysfunction: Insights on the role in neurodegeneration , 2009, Brain Research Bulletin.

[90]  J. Uslaner,et al.  Dose-dependent effect of CDPPB, the mGluR5 positive allosteric modulator, on recognition memory is associated with GluR1 and CREB phosphorylation in the prefrontal cortex and hippocampus , 2009, Neuropharmacology.

[91]  S. Dolan,et al.  The selective metabotropic glutamate receptor 7 allosteric agonist AMN082 inhibits inflammatory pain-induced and incision-induced hypersensitivity in rat , 2009, Behavioural pharmacology.

[92]  P. Gubellini,et al.  Electrophysiological and behavioral evidence that modulation of metabotropic glutamate receptor 4 with a new agonist reverses experimental parkinsonism , 2009, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

[93]  Kari A. Johnson,et al.  Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4). , 2009, Bioorganic & medicinal chemistry letters.

[94]  S. Ozaki,et al.  Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one , 2009, Neuropharmacology.

[95]  P Jeffrey Conn,et al.  Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). , 2009, Journal of medicinal chemistry.

[96]  C. Lindsley,et al.  Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines. , 2009, Journal of medicinal chemistry.

[97]  F. Weiss,et al.  Dissociation of the Effects of MTEP [3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]piperidine] on Conditioned Reinstatement and Reinforcement: Comparison between Cocaine and a Conventional Reinforcer , 2009, Journal of Pharmacology and Experimental Therapeutics.

[98]  J. Tack,et al.  A proof-of-concept study evaluating the effect of ADX10059, a metabotropic glutamate receptor-5 negative allosteric modulator, on acid exposure and symptoms in gastro-oesophageal reflux disease , 2009, Gut.

[99]  P. Gubellini,et al.  Metabotropic glutamate receptor subtype 4 selectively modulates both glutamate and GABA transmission in the striatum: implications for Parkinson’s disease treatment , 2009, Journal of neurochemistry.

[100]  M. Olive,et al.  Positive Allosteric Modulation of mGluR5 Receptors Facilitates Extinction of a Cocaine Contextual Memory , 2009, Biological Psychiatry.

[101]  M. Olive,et al.  mGluR5 Antagonism Attenuates Methamphetamine Reinforcement and Prevents Reinstatement of Methamphetamine-Seeking Behavior in Rats , 2009, Neuropsychopharmacology.

[102]  M. Foster Olive,et al.  mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning , 2009, Neuropsychopharmacology.

[103]  U. Holzgrabe,et al.  Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity , 2009, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.

[104]  D. Nguyen,et al.  A pilot open label, single dose trial of fenobam in adults with fragile X syndrome , 2009, Journal of Medical Genetics.

[105]  F. Liu,et al.  ADX47273 [S-(4-Fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: A Novel Metabotropic Glutamate Receptor 5-Selective Positive Allosteric Modulator with Preclinical Antipsychotic-Like and Procognitive Activities , 2008, Journal of Pharmacology and Experimental Therapeutics.

[106]  Kari A. Johnson,et al.  Discovery, Characterization, and Antiparkinsonian Effect of Novel Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4 , 2008, Molecular Pharmacology.

[107]  Arthur Christopoulos,et al.  A Novel Mechanism of G Protein-coupled Receptor Functional Selectivity , 2008, Journal of Biological Chemistry.

[108]  V. Neugebauer,et al.  Group III mGluR7 and mGluR8 in the amygdala differentially modulate nocifensive and affective pain behaviors , 2008, Neuropharmacology.

[109]  J. Cryan,et al.  Selective activation of metabotropic G-protein-coupled glutamate 7 receptor elicits anxiolytic-like effects in mice by modulating GABAergic neurotransmission , 2008, Behavioural pharmacology.

[110]  J. Erickson,et al.  Efficacy and Tolerability of an mGlu2/3 Agonist in the Treatment of Generalized Anxiety Disorder , 2008, Neuropsychopharmacology.

[111]  D. Sheffler,et al.  Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells , 2008, Neuropharmacology.

[112]  M. Amalric,et al.  Functional interaction between adenosine A2A and group III metabotropic glutamate receptors to reduce parkinsonian symptoms in rats , 2008, Neuropharmacology.

[113]  C. Lüscher,et al.  Mechanisms of synaptic depression triggered by metabotropic glutamate receptors , 2008, Cellular and Molecular Life Sciences.

[114]  L. Lubbers,et al.  Transposition of Three Amino Acids Transforms the Human Metabotropic Glutamate Receptor (mGluR)-3-Positive Allosteric Modulation Site to mGluR2, and Additional Characterization of the mGluR2-Positive Allosteric Modulation Site , 2008, Journal of Pharmacology and Experimental Therapeutics.

[115]  D. Schoepp,et al.  Evidence for the Role of Metabotropic Glutamate (mGlu)2 Not mGlu3 Receptors in the Preclinical Antipsychotic Pharmacology of the mGlu2/3 Receptor Agonist (–)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic Acid (LY404039) , 2008, Journal of Pharmacology and Experimental Therapeutics.

[116]  A. Eschalier,et al.  Group III metabotropic glutamate receptors inhibit hyperalgesia in animal models of inflammation and neuropathic pain , 2008, Pain.

[117]  C. Mulle,et al.  Presynaptic glutamate receptors: physiological functions and mechanisms of action , 2008, Nature Reviews Neuroscience.

[118]  D. Javitt,et al.  Circuit-based framework for understanding neurotransmitter and risk gene interactions in schizophrenia , 2008, Trends in Neurosciences.

[119]  Stephen T Warren,et al.  Fragile X syndrome , 2008, European Journal of Human Genetics.

[120]  C. Tamminga,et al.  Schizophrenia: moving beyond monoamine antagonists. , 2008, Molecular interventions.

[121]  P. Jeffrey Conn,et al.  N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) Acts through a Novel Site as a Positive Allosteric Modulator of Group 1 Metabotropic Glutamate Receptors , 2008, Molecular Pharmacology.

[122]  H. Lavreysen,et al.  Therapeutic potential of group III metabotropic glutamate receptors. , 2008, Current medicinal chemistry.

[123]  S. Duty,et al.  Group III metabotropic glutamate receptors act as hetero-receptors modulating evoked GABA release in the globus pallidus in vivo. , 2008, European journal of pharmacology.

[124]  R. Tatarelli,et al.  Synergism between fluoxetine and the mGlu2/3 receptor agonist, LY379268, in an in vitro model for antidepressant drug-induced neurogenesis , 2008, Neuropharmacology.

[125]  Mark F. Bear,et al.  Correction of Fragile X Syndrome in Mice , 2007, Neuron.

[126]  T. Kenakin Functional Selectivity through Protean and Biased Agonism: Who Steers the Ship? , 2007, Molecular Pharmacology.

[127]  Jack J. Chen,et al.  Pharmacotherapy for Parkinson's Disease , 2007, Pharmacotherapy.

[128]  G. Carmignoto,et al.  Enhanced Astrocytic Ca2+ Signals Contribute to Neuronal Excitotoxicity after Status Epilepticus , 2007, The Journal of Neuroscience.

[129]  G. Lynch,et al.  Brain-Derived Neurotrophic Factor Rescues Synaptic Plasticity in a Mouse Model of Fragile X Syndrome , 2007, The Journal of Neuroscience.

[130]  B. Moghaddam,et al.  Positive Allosteric Modulation of Metabotropic Glutamate 5 (mGlu5) Receptors Reverses N-Methyl-D-Aspartate Antagonist-Induced Alteration of Neuronal Firing in Prefrontal Cortex , 2007, Biological Psychiatry.

[131]  S. Mosolov,et al.  Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: a randomized Phase 2 clinical trial , 2007, Nature Medicine.

[132]  Meixiang Yu Recent developments of the PET imaging agents for metabotropic glutamate receptor subtype 5. , 2007, Current topics in medicinal chemistry.

[133]  M. Liechti,et al.  Metabotropic Glutamate 2/3 Receptors in the Ventral Tegmental Area and the Nucleus Accumbens Shell Are Involved in Behaviors Relating to Nicotine Dependence , 2007, The Journal of Neuroscience.

[134]  Z. Xiang,et al.  A Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 2 Blocks a Hallucinogenic Drug Model of Psychosis , 2007, Molecular Pharmacology.

[135]  M. Bouvier,et al.  The evasive nature of drug efficacy: implications for drug discovery. , 2007, Trends in pharmacological sciences.

[136]  P. Sexton,et al.  Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology. , 2007, Trends in pharmacological sciences.

[137]  Valerie Treyer,et al.  Evaluation of the Metabotropic Glutamate Receptor Subtype 5 Using PET and 11C-ABP688: Assessment of Methods , 2007, Journal of Nuclear Medicine.

[138]  P. Conn,et al.  A Novel Family of Potent Negative Allosteric Modulators of Group II Metabotropic Glutamate Receptors , 2007, Journal of Pharmacology and Experimental Therapeutics.

[139]  M. Amalric,et al.  Targeting Group III Metabotropic Glutamate Receptors Produces Complex Behavioral Effects in Rodent Models of Parkinson's Disease , 2007, The Journal of Neuroscience.

[140]  Hisashi Ohta,et al.  Pharmacological Characterization of a New, Orally Active and Potent Allosteric Metabotropic Glutamate Receptor 1 Antagonist, 4-[1-(2-Fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide (FTIDC) , 2007, Journal of Pharmacology and Experimental Therapeutics.

[141]  J. Schkeryantz,et al.  Prospects for metabotropic glutamate 1 receptor antagonists in the treatment of neuropathic pain. , 2007, Journal of medicinal chemistry.

[142]  J. Pin,et al.  Interaction of Novel Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 with the Negative Allosteric Antagonist Site Is Required for Potentiation of Receptor Responses , 2007, Molecular Pharmacology.

[143]  K. Perry,et al.  In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonist LY404039 in animal models of psychiatric disorders , 2007, Psychopharmacology.

[144]  Takanori Muto,et al.  Structures of the extracellular regions of the group II/III metabotropic glutamate receptors , 2007, Proceedings of the National Academy of Sciences.

[145]  C. Lindsley,et al.  Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. , 2007, Bioorganic & medicinal chemistry letters.

[146]  J. Wroblewski,et al.  Cyclothiazide selectively inhibits mGluR1 receptors interacting with a common allosteric site for non-competitive antagonists , 2007, Neuropharmacology.

[147]  Y. Shaham,et al.  Systemic and Central Amygdala Injections of the mGluR2/3 Agonist LY379268 Attenuate the Expression of Incubation of Cocaine Craving , 2007, Biological Psychiatry.

[148]  Mark E. Schmidt,et al.  Human PET studies of metabotropic glutamate receptor subtype 5 with 11C-ABP688. , 2007, Journal of nuclear medicine : official publication, Society of Nuclear Medicine.

[149]  P. Popik,et al.  Antidepressant-like effects of mGluR1 and mGluR5 antagonists in the rat forced swim and the mouse tail suspension tests , 2007, European Neuropsychopharmacology.

[150]  M. Liechti,et al.  Interactive effects of the mGlu5 receptor antagonist MPEP and the mGlu2/3 receptor antagonist LY341495 on nicotine self-administration and reward deficits associated with nicotine withdrawal in rats. , 2007, European journal of pharmacology.

[151]  Arthur Christopoulos,et al.  Functional Selectivity and Classical Concepts of Quantitative Pharmacology , 2007, Journal of Pharmacology and Experimental Therapeutics.

[152]  K. Szumlinski,et al.  Behavioral and neurochemical interactions between Group 1 mGluR antagonists and ethanol: potential insight into their anti-addictive properties. , 2006, Drug and alcohol dependence.

[153]  D. Balschun,et al.  Allosteric enhancement of metabotropic glutamate receptor 5 function promotes spatial memory , 2006, Neuroscience.

[154]  Y. Shaham,et al.  Activation of Group II Metabotropic Glutamate Receptors in the Nucleus Accumbens Shell Attenuates Context-Induced Relapse to Heroin Seeking , 2006, Neuropsychopharmacology.

[155]  Xia Li,et al.  Metabotropic Glutamate 5 Receptor Antagonism Is Associated with Antidepressant-Like Effects in Mice , 2006, Journal of Pharmacology and Experimental Therapeutics.

[156]  S. Gobbo,et al.  Astrocytic Glutamate Is Not Necessary for the Generation of Epileptiform Neuronal Activity in Hippocampal Slices , 2006, The Journal of Neuroscience.

[157]  G. Labesse,et al.  Coupling of Agonist Binding to Effector Domain Activation in Metabotropic Glutamate-like Receptors* , 2006, Journal of Biological Chemistry.

[158]  R. Chang,et al.  Design, Synthesis, and In Vivo Efficacy of Glycine Transporter‐1 (GlyT1) Inhibitors Derived from a Series of [4‐Phenyl‐1‐(propylsulfonyl)piperidin‐4‐yl]methyl Benzamides , 2006, ChemMedChem.

[159]  R. Spealman,et al.  Pharmacological Stimulation of Group II Metabotropic Glutamate Receptors Reduces Cocaine Self-Administration and Cocaine-Induced Reinstatement of Drug Seeking in Squirrel Monkeys , 2006, Journal of Pharmacology and Experimental Therapeutics.

[160]  Paul J Carlson,et al.  A randomized trial of an N-methyl-D-aspartate antagonist in treatment-resistant major depression. , 2006, Archives of general psychiatry.

[161]  P. Conn,et al.  A Novel Class of Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 1 Interact with a Site Distinct from That of Negative Allosteric Modulators , 2006, Molecular Pharmacology.

[162]  Francesco Ferraguti,et al.  Metabotropic glutamate receptors , 2006, Cell and Tissue Research.

[163]  F. Nicoletti,et al.  Pharmacological Activation of mGlu4 Metabotropic Glutamate Receptors Reduces Nigrostriatal Degeneration in Mice Treated with 1-Methyl-4-Phenyl-1,2,3,6-Tetrahydropyridine , 2006, The Journal of Neuroscience.

[164]  Martin Stahl,et al.  Comparison of the binding pockets of two chemically unrelated allosteric antagonists of the mGlu5 receptor and identification of crucial residues involved in the inverse agonism of MPEP , 2006, Journal of neurochemistry.

[165]  P. Conn,et al.  Biphenyl-indanone A, a Positive Allosteric Modulator of the Metabotropic Glutamate Receptor Subtype 2, Has Antipsychotic- and Anxiolytic-Like Effects in Mice , 2006, Journal of Pharmacology and Experimental Therapeutics.

[166]  J. Peters,et al.  The group II metabotropic glutamate receptor agonist, LY379268, inhibits both cocaine- and food-seeking behavior in rats , 2006, Psychopharmacology.

[167]  S. Chaki,et al.  An mGluR2/3 antagonist, MGS0039, exerts antidepressant and anxiolytic effects in behavioral models in rats , 2006, Psychopharmacology.

[168]  Christian Steinhäuser,et al.  Astrocyte dysfunction in neurological disorders: a molecular perspective , 2006, Nature Reviews Neuroscience.

[169]  K. Chaudhuri,et al.  Non-motor symptoms of Parkinson's disease: diagnosis and management , 2006, The Lancet Neurology.

[170]  P. Conn,et al.  Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors. , 2006, Current opinion in pharmacology.

[171]  Andreas Mühlemann,et al.  Determination of key amino acids implicated in the actions of allosteric modulation by 3,3'-difluorobenzaldazine on rat mGlu5 receptors. , 2006, European journal of pharmacology.

[172]  K. Hsu,et al.  Sustained activation of metabotropic glutamate receptor 5 and protein tyrosine phosphatases mediate the expression of (S)‐3,5‐dihydroxyphenylglycine‐induced long‐term depression in the hippocampal CA1 region , 2006, Journal of neurochemistry.

[173]  I. Mansuy,et al.  NMDA-induced potentiation of mGluR5 is mediated by activation of protein phosphatase 2B/calcineurin , 2005, Neuropharmacology.

[174]  P. Hyytiä,et al.  Suppression of alcohol self-administration and cue-induced reinstatement of alcohol seeking by the mGlu2/3 receptor agonist LY379268 and the mGlu8 receptor agonist (S)-3,4-DCPG. , 2005, European journal of pharmacology.

[175]  J. Cryan,et al.  A selective metabotropic glutamate receptor 7 agonist: activation of receptor signaling via an allosteric site modulates stress parameters in vivo. , 2005, Proceedings of the National Academy of Sciences of the United States of America.

[176]  M. Tranfaglia,et al.  Suppression of two major Fragile X Syndrome mouse model phenotypes by the mGluR5 antagonist MPEP , 2005, Neuropharmacology.

[177]  P. Jeffrey Conn,et al.  A Close Structural Analog of 2-Methyl-6-(phenylethynyl)-pyridine Acts as a Neutral Allosteric Site Ligand on Metabotropic Glutamate Receptor Subtype 5 and Blocks the Effects of Multiple Allosteric Modulators , 2005, Molecular Pharmacology.

[178]  P. Conn,et al.  Allosteric Potentiators of Metabotropic Glutamate Receptor Subtype 5 Have Differential Effects on Different Signaling Pathways in Cortical Astrocytes , 2005, Journal of Pharmacology and Experimental Therapeutics.

[179]  P. Conn,et al.  A Selective Allosteric Potentiator of Metabotropic Glutamate (mGlu) 2 Receptors Has Effects Similar to an Orthosteric mGlu2/3 Receptor Agonist in Mouse Models Predictive of Antipsychotic Activity , 2005, Journal of Pharmacology and Experimental Therapeutics.

[180]  A. Christopoulos,et al.  Allosteric Modulation of the Cannabinoid CB1 Receptor , 2005, Molecular Pharmacology.

[181]  Jens-Uwe Peters,et al.  Fenobam: A Clinically Validated Nonbenzodiazepine Anxiolytic Is a Potent, Selective, and Noncompetitive mGlu5 Receptor Antagonist with Inverse Agonist Activity , 2005, Journal of Pharmacology and Experimental Therapeutics.

[182]  X. Langlois,et al.  Metabotropic glutamate receptor 1 blockade impairs acquisition and retention in a spatial Water maze task , 2005, Behavioural Brain Research.

[183]  P. Jeffrey Conn,et al.  Metabotropic glutamate receptors in the basal ganglia motor circuit , 2005, Nature Reviews Neuroscience.

[184]  Seiji Tamura,et al.  Radioligand Binding Properties and Pharmacological Characterization of 6-Amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide (YM-298198), a High-Affinity, Selective, and Noncompetitive Antagonist of Metabotropic Glutamate Receptor Type 1 , 2005, Journal of Pharmacology and Experimental Therapeutics.

[185]  L. Bristow,et al.  Benzazoles as allosteric potentiators of metabotropic glutamate receptor 2 (mGluR2): efficacy in an animal model for schizophrenia. , 2005, Bioorganic & medicinal chemistry letters.

[186]  W. Schmidt,et al.  Effects of MPEP on expression of food‐, MDMA‐ or amphetamine‐conditioned place preference in rats , 2005, Addiction biology.

[187]  M. Śmiałowska,et al.  A slowly developing dysfunction of dopaminergic nigrostriatal neurons induced by long‐term paraquat administration in rats: an animal model of preclinical stages of Parkinson's disease? , 2005, The European journal of neuroscience.

[188]  Andrzej Pilc,et al.  MTEP, a new selective antagonist of the metabotropic glutamate receptor subtype 5 (mGluR5), produces antiparkinsonian-like effects in rats , 2005, Neuropharmacology.

[189]  Karolina Nilsson,et al.  Recent advances in non-competitive mGlu5 receptor antagonists and their potential therapeutic applications. , 2005, Current topics in medicinal chemistry.

[190]  F. Nicoletti,et al.  Metabotropic glutamate receptors and neuroadaptation to antidepressants: imipramine‐induced down‐regulation of β‐adrenergic receptors in mice treated with metabotropic glutamate 2/3 receptor ligands , 2005, Journal of neurochemistry.

[191]  W. Danysz,et al.  Anxiolytic-like effects of mGlu1 and mGlu5 receptor antagonists in rats. , 2005, European journal of pharmacology.

[192]  C. Lindsley,et al.  A Novel Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Has in Vivo Activity and Antipsychotic-Like Effects in Rat Behavioral Models , 2005, Journal of Pharmacology and Experimental Therapeutics.

[193]  A. Pinkerton,et al.  Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators. , 2005, Bioorganic & medicinal chemistry letters.

[194]  W. Schmidt,et al.  Effects of mGlu1 and mGlu5 receptor antagonists on negatively reinforced learning , 2005, Behavioural pharmacology.

[195]  E. Nisenbaum,et al.  Metabotropic glutamate 2 receptor potentiators: receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model(s) , 2005, Psychopharmacology.

[196]  C. Swanson,et al.  Metabotropic glutamate receptors as novel targets for anxiety and stress disorders , 2005, Nature Reviews Drug Discovery.

[197]  R. Wouters,et al.  Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists. , 2005, Journal of medicinal chemistry.

[198]  J. Feldon,et al.  Effects of the mGluR2/3 agonist LY354740 on computerized tasks of attention and working memory in marmoset monkeys , 2005, Psychopharmacology.

[199]  X. Langlois,et al.  JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist , 2004, Neuropharmacology.

[200]  P Jeffrey Conn,et al.  Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo. , 2004, Journal of medicinal chemistry.

[201]  M. Pilla,et al.  Antagonism at metabotropic glutamate 5 receptors inhibits nicotine- and cocaine-taking behaviours and prevents nicotine-triggered relapse to nicotine-seeking. , 2004, European journal of pharmacology.

[202]  Qi Wu,et al.  NCD3G: a novel nine-cysteine domain in family 3 GPCRs , 2004 .

[203]  I. Kola,et al.  Can the pharmaceutical industry reduce attrition rates? , 2004, Nature Reviews Drug Discovery.

[204]  Mark F Bear,et al.  The mGluR theory of fragile X mental retardation , 2004, Trends in Neurosciences.

[205]  V. Neugebauer,et al.  Enhanced group III mGluR-mediated inhibition of pain-related synaptic plasticity in the amygdala , 2004, Neuropharmacology.

[206]  P Jeffrey Conn,et al.  A Novel Selective Allosteric Modulator Potentiates the Activity of Native Metabotropic Glutamate Receptor Subtype 5 in Rat Forebrain , 2004, Journal of Pharmacology and Experimental Therapeutics.

[207]  R. Spanagel,et al.  mGluR5 Antagonist MPEP Reduces Ethanol-Seeking and Relapse Behavior , 2004, Neuropsychopharmacology.

[208]  P. Conn,et al.  The mGluR5 antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) potentiates PCP-induced cognitive deficits in rats , 2004, Psychopharmacology.

[209]  S. Nakanishi,et al.  MGS0039: a potent and selective group II metabotropic glutamate receptor antagonist with antidepressant-like activity , 2004, Neuropharmacology.

[210]  B. Szewczyk,et al.  Group III mGlu receptor agonists produce anxiolytic- and antidepressant-like effects after central administration in rats , 2004, Neuropharmacology.

[211]  S. Duty,et al.  Activation of group III metabotropic glutamate receptors in selected regions of the basal ganglia alleviates akinesia in the reserpine‐treated rat , 2004, British journal of pharmacology.

[212]  H. Kita,et al.  Activation of group III metabotropic glutamate receptors presynaptically reduces both GABAergic and glutamatergic transmission in the rat globus pallidus , 2003, Neuroscience.

[213]  Francine Acher,et al.  Heptahelical domain of metabotropic glutamate receptor 5 behaves like rhodopsin-like receptors , 2003, Proceedings of the National Academy of Sciences of the United States of America.

[214]  I. Vranesic,et al.  (−)-PHCCC, a positive allosteric modulator of mGluR4: characterization, mechanism of action, and neuroprotection , 2003, Neuropharmacology.

[215]  A. Dilella,et al.  Allosteric modulation of group III metabotropic glutamate receptor 4: A potential approach to Parkinson's disease treatment , 2003, Proceedings of the National Academy of Sciences of the United States of America.

[216]  P. Malherbe,et al.  Mutational analysis and molecular modeling of the binding pocket of the metabotropic glutamate 5 receptor negative modulator 2-methyl-6-(phenylethynyl)-pyridine. , 2003, Molecular pharmacology.

[217]  L. Bristow,et al.  Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2. , 2003, Molecular pharmacology.

[218]  M. Amalric,et al.  Metabotropic Glutamate 5 Receptor Blockade Alleviates Akinesia by Normalizing Activity of Selective Basal-Ganglia Structures in Parkinsonian Rats , 2003, The Journal of Neuroscience.

[219]  P Jeffrey Conn,et al.  A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. , 2003, Molecular pharmacology.

[220]  P Jeffrey Conn,et al.  Group III Metabotropic Glutamate Receptor-Mediated Modulation of the Striatopallidal Synapse , 2003, The Journal of Neuroscience.

[221]  N. Cosford,et al.  In vivo receptor occupancy of mGlu5 receptor antagonists using the novel radioligand [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine). , 2003, European journal of pharmacology.

[222]  D. Lorrain,et al.  Group II mGlu Receptor Activation Suppresses Norepinephrine Release in the Ventral Hippocampus and Locomotor Responses to Acute Ketamine Challenge , 2003, Neuropsychopharmacology.

[223]  Olga V. Demler,et al.  The epidemiology of major depressive disorder: results from the National Comorbidity Survey Replication (NCS-R). , 2003, JAMA.

[224]  P. Kelly,et al.  Antidepressant and anxiolytic‐like effects in mice lacking the group III metabotropic glutamate receptor mGluR7 , 2003, The European journal of neuroscience.

[225]  Xavier Langlois,et al.  [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists. , 2003, Molecular pharmacology.

[226]  J. Kew,et al.  Mutational Analysis and Molecular Modeling of the Allosteric Binding Site of a Novel, Selective, Noncompetitive Antagonist of the Metabotropic Glutamate 1 Receptor* , 2003, The Journal of Biological Chemistry.

[227]  J. M. Mathiesen,et al.  Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB‐1893 and MPEP , 2003, British journal of pharmacology.

[228]  N. Cosford,et al.  [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor. , 2003, Bioorganic & medicinal chemistry letters.

[229]  Arne Schousboe,et al.  Role of Astrocytes in the Maintenance and Modulation of Glutamatergic and GABAergic Neurotransmission , 2003, Neurochemical Research.

[230]  Mark Washburn,et al.  3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. , 2003, Journal of medicinal chemistry.

[231]  L. Levine,et al.  LY354740, an mGlu2/3 Receptor Agonist as a Novel Approach to Treat Anxiety/Stress , 2003, Stress.

[232]  Thomas Knöpfel,et al.  Book Review: Metabotropic Glutamate Receptors: Electrical and Chemical Signaling Properties , 2002, The Neuroscientist : a review journal bringing neurobiology, neurology and psychiatry.

[233]  Nicholas D. P. Cosford,et al.  [3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine Binding to Metabotropic Glutamate Receptor Subtype 5 in Rodent Brain: In Vitro and in Vivo Characterization , 2002, Journal of Pharmacology and Experimental Therapeutics.

[234]  P. Popik,et al.  Morphine conditioned reward is inhibited by MPEP, the mGluR5 antagonist , 2002, Neuropharmacology.

[235]  Michael Davis,et al.  Behavioral and Neural Analysis of Extinction , 2002, Neuron.

[236]  D. Balschun,et al.  Inhibition of mGluR5 blocks hippocampal LTP in vivo and spatial learning in rats , 2002, Pharmacology Biochemistry and Behavior.

[237]  E. Meli,et al.  Activation of mGlu1 but not mGlu5 metabotropic glutamate receptors contributes to postischemic neuronal injury in vitro and in vivo , 2002, Pharmacology Biochemistry and Behavior.

[238]  P. Saggau,et al.  Modulation of Presynaptic Calcium Transients by Metabotropic Glutamate Receptor Activation: A Differential Role in Acute Depression of Synaptic Transmission and Long-Term Depression , 2002, The Journal of Neuroscience.

[239]  D. Schoepp,et al.  Increased anxiety-related behavior in mice deficient for metabotropic glutamate 8 (mGlu8) receptor , 2002, Neuropharmacology.

[240]  L. Prézeau,et al.  Closure of the Venus flytrap module of mGlu8 receptor and the activation process: Insights from mutations converting antagonists into agonists , 2002, Proceedings of the National Academy of Sciences of the United States of America.

[241]  V. Neugebauer Metabotropic glutamate receptors – important modulators of nociception and pain behavior , 2002, Pain.

[242]  M. Amalric,et al.  Chronic But Not Acute Treatment with a Metabotropic Glutamate 5 Receptor Antagonist Reverses the Akinetic Deficits in a Rat Model of Parkinsonism , 2002, The Journal of Neuroscience.

[243]  Joseph E LeDoux,et al.  The Group I Metabotropic Glutamate Receptor mGluR5 Is Required for Fear Memory Formation and Long-Term Potentiation in the Lateral Amygdala , 2002, The Journal of Neuroscience.

[244]  L. Prézeau,et al.  A model for the functioning of family 3 GPCRs. , 2002, Trends in pharmacological sciences.

[245]  Mark F. Bear,et al.  Altered synaptic plasticity in a mouse model of fragile X mental retardation , 2002, Proceedings of the National Academy of Sciences of the United States of America.

[246]  P. Conn,et al.  Distinct physiological roles of the Gq‐coupled metabotropic glutamate receptors co‐expressed in the same neuronal populations , 2002, Journal of cellular physiology.

[247]  N. Kunishima,et al.  Structural views of the ligand-binding cores of a metabotropic glutamate receptor complexed with an antagonist and both glutamate and Gd3+ , 2002, Proceedings of the National Academy of Sciences of the United States of America.

[248]  Fabrizio Gasparini,et al.  [(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5. , 2002, Bioorganic & medicinal chemistry letters.

[249]  P. Conn,et al.  Direct and indirect modulation of the N-methyl D-aspartate receptor. , 2002, Current drug targets. CNS and neurological disorders.

[250]  W. Spooren,et al.  Pharmacological and endocrinological characterisation of stress-induced hyperthermia in singly housed mice using classical and candidate anxiolytics (LY314582, MPEP and NKP608). , 2002, European journal of pharmacology.

[251]  J. Kemp,et al.  Positive allosteric modulators of metabotropic glutamate 1 receptor: Characterization, mechanism of action, and binding site , 2001, Proceedings of the National Academy of Sciences of the United States of America.

[252]  Andrzej Pilc,et al.  The antianxiety-like effects of antagonists of group I and agonists of group II and III metabotropic glutamate receptors after intrahippocampal administration , 2001, Psychopharmacology.

[253]  G Bernardi,et al.  Metabotropic glutamate receptor 5 mediates the potentiation of N-methyl-D-aspartate responses in medium spiny striatal neurons , 2001, Neuroscience.

[254]  F. Nicoletti,et al.  Metabotropic Glutamate Receptor Subtypes as Targets for Neuroprotective Drugs , 2001, Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism.

[255]  Dana C Crawford,et al.  FMR1 and the fragile X syndrome: Human genome epidemiology review , 2001, Genetics in Medicine.

[256]  S. Traynelis,et al.  Metabotropic Glutamate Receptors 1 and 5 Differentially Regulate CA1 Pyramidal Cell Function , 2001, The Journal of Neuroscience.

[257]  F. Conquet,et al.  Reinforcing and locomotor stimulant effects of cocaine are absent in mGluR5 null mutant mice , 2001, Nature Neuroscience.

[258]  F. Nicoletti,et al.  Retracted: Neuroprotection mediated by glial group‐II metabotropic glutamate receptors requires the activation of the MAP kinase and the phosphatidylinositol‐3‐kinase pathways , 2001, Journal of neurochemistry.

[259]  D C Teller,et al.  Advances in determination of a high-resolution three-dimensional structure of rhodopsin, a model of G-protein-coupled receptors (GPCRs). , 2001, Biochemistry.

[260]  M. Bear,et al.  Chemical induction of mGluR5- and protein synthesis--dependent long-term depression in hippocampal area CA1. , 2001, Journal of neurophysiology.

[261]  M. Koch,et al.  The metabotropic glutamate receptor antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) blocks fear conditioning in rats , 2001, Neuropharmacology.

[262]  K. Perry,et al.  Acute increases in monoamine release in the rat prefrontal cortex by the mGlu2/3 agonist LY379268 are similar in profile to risperidone, not locally mediated, and can be elicited in the presence of uptake blockade , 2001, Neuropharmacology.

[263]  S. Oliet,et al.  Control of Glutamate Clearance and Synaptic Efficacy by Glial Coverage of Neurons , 2001, Science.

[264]  P. Conn,et al.  Activation of group III mGluRs inhibits GABAergic and glutamatergic transmission in the substantia nigra pars reticulata. , 2001, Journal of neurophysiology.

[265]  L. Prézeau,et al.  BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity. , 2001, Molecular pharmacology.

[266]  F. Gasparini,et al.  Discovery and characterization of non-competitive antagonists of group I metabotropic glutamate receptors. , 2001, Farmaco.

[267]  P. Calabresi,et al.  Functional coexpression of excitatory mGluR1 and mGluR5 on striatal cholinergic interneurons , 2001, Neuropharmacology.

[268]  J. Mateos,et al.  Immunoreactivity for the group III metabotropic glutamate receptor subtype mGluR4a in the superficial laminae of the rat spinal dorsal horn , 2001, The Journal of comparative neurology.

[269]  F. Moroni,et al.  Activation of type 5 metabotropic glutamate receptors enhances NMDA responses in mice cortical wedges , 2001, British journal of pharmacology.

[270]  D. Hall,et al.  Modeling the functional effects of allosteric modulators at pharmacological receptors: an extension of the two-state model of receptor activation. , 2000, Molecular pharmacology.

[271]  W. Spooren,et al.  Anxiolytic-like effects of the prototypical metabotropic glutamate receptor 5 antagonist 2-methyl-6-(phenylethynyl)pyridine in rodents. , 2000, The Journal of pharmacology and experimental therapeutics.

[272]  W. Willis,et al.  Groups II and III metabotropic glutamate receptors differentially modulate brief and prolonged nociception in primate STT cells. , 2000, Journal of neurophysiology.

[273]  S. Nakanishi,et al.  Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists. , 2000, Journal of medicinal chemistry.

[274]  Y. Smith,et al.  Activation of Metabotropic Glutamate Receptor 5 Has Direct Excitatory Effects and Potentiates NMDA Receptor Currents in Neurons of the Subthalamic Nucleus , 2000, The Journal of Neuroscience.

[275]  F. Gasparini,et al.  The Non-competitive Antagonists 2-Methyl-6-(phenylethynyl)pyridine and 7-Hydroxyiminocyclopropan[b]chromen-1a-carboxylic Acid Ethyl Ester Interact with Overlapping Binding Pockets in the Transmembrane Region of Group I Metabotropic Glutamate Receptors* , 2000, The Journal of Biological Chemistry.

[276]  S. Nakanishi,et al.  Structural basis of glutamate recognition by a dimeric metabotropic glutamate receptor , 2000, Nature.

[277]  F. Gasparini,et al.  Chiral resolution, pharmacological characterization, and receptor docking of the noncompetitive mGlu1 receptor antagonist (+/-)-2-hydroxyimino- 1a, 2-dihydro-1H-7-oxacyclopropa[b]naphthalene-7a-carboxylic acid ethyl ester. , 2000, Journal of medicinal chemistry.

[278]  R. Swanson,et al.  Astrocyte glutamate transport: Review of properties, regulation, and physiological functions , 2000, Glia.

[279]  D. Schoepp,et al.  Regulation of Neurotransmitter Release by Metabotropic Glutamate Receptors , 2000, Journal of neurochemistry.

[280]  Z. Bortolotto,et al.  A novel, competitive mGlu5 receptor antagonist (LY344545) blocks DHPG‐induced potentiation of NMDA responses but not the induction of LTP in rat hippocampal slices , 2000 .

[281]  K. Palczewski,et al.  Crystal Structure of Rhodopsin: A G‐Protein‐Coupled Receptor , 2002, Chembiochem : a European journal of chemical biology.

[282]  John H Krystal,et al.  Antidepressant effects of ketamine in depressed patients , 2000, Biological Psychiatry.

[283]  P. Krogsgaard‐Larsen,et al.  Interaction of CPCCOEt with a chimeric mGlu1b and calcium sensing receptor. , 1999, Neuroreport.

[284]  M. Ehlers,et al.  Synapse structure: Glutamate receptors connected by the shanks , 1999, Current Biology.

[285]  H. Kimelberg,et al.  mGluR3 and mGluR5 are the predominant metabotropic glutamate receptor mRNAs expressed in hippocampal astrocytes acutely isolated from young rats , 1999, Journal of neuroscience research.

[286]  F. Bordi,et al.  Potentiation of NMDA and AMPA responses by the specific mGluR5 agonist CHPG in spinal cord motoneurons , 1999, Neuropharmacology.

[287]  Roland Heckendorn,et al.  2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist , 1999, Neuropharmacology.

[288]  D. Schoepp,et al.  The metabotropic glutamate 2/3 receptor agonists LY354740 and LY379268 selectively attenuate phencyclidine versus d-amphetamine motor behaviors in rats. , 1999, The Journal of pharmacology and experimental therapeutics.

[289]  F. Gasparini,et al.  SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5. , 1999, The Journal of pharmacology and experimental therapeutics.

[290]  S. Heinemann,et al.  Activation of NMDA receptors reverses desensitization of mGluR5 in native and recombinant systems , 1999, Nature Neuroscience.

[291]  F. Gasparini,et al.  CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding. , 1999, Molecular pharmacology.

[292]  R. Anwyl Metabotropic glutamate receptors: electrophysiological properties and role in plasticity , 1999, Brain Research Reviews.

[293]  F. Nicoletti,et al.  Neuroprotection by Glial Metabotropic Glutamate Receptors Is Mediated by Transforming Growth Factor-β , 1998, The Journal of Neuroscience.

[294]  B. Moghaddam,et al.  Reversal of phencyclidine effects by a group II metabotropic glutamate receptor agonist in rats. , 1998, Science.

[295]  D. Schoepp,et al.  LY354740: a metabotropic glutamate receptor agonist which ameliorates symptoms of nicotine withdrawal in rats , 1997, Neuropharmacology.

[296]  T. Pozzan,et al.  Intracellular Calcium Oscillations in Astrocytes: A Highly Plastic, Bidirectional Form of Communication between Neurons and Astrocytes In Situ , 1997, The Journal of Neuroscience.

[297]  S. Nakanishi,et al.  The Metabotropic Glutamate Receptor mGluR5 Induces Calcium Oscillations in Cultured Astrocytes via Protein Kinase C Phosphorylation , 1997, Journal of neurochemistry.

[298]  J. Roder,et al.  Mice Lacking Metabotropic Glutamate Receptor 5 Show Impaired Learning and Reduced CA1 Long-Term Potentiation (LTP) But Normal CA3 LTP , 1997, The Journal of Neuroscience.

[299]  H. Schild,et al.  SOME QUANTITATIVE USES OF DRUG ANTAGONISTS , 1997, British journal of pharmacology and chemotherapy.

[300]  Andrzej Pilc,et al.  The anxiolytic-like effect of metabotropic glutamate receptor antagonists after intrahippocampal injection in rats. , 1997, European journal of pharmacology.

[301]  C. Romano,et al.  Metabotropic Glutamate Receptor 5 Is a Disulfide-linked Dimer* , 1996, The Journal of Biological Chemistry.

[302]  Atsuko Fukunaga,et al.  A novel class of antagonists for metabotropic glutamate receptors, 7-(Hydroxyimino)cyclopropa[b]chromen-1a-carboxylates , 1996 .

[303]  T. Knöpfel,et al.  The agonist selectivity of a class III metabotropic glutamate receptor, human mGluR4a, is determined by the N-terminal extracellular domain , 1995, Neuroreport.

[304]  A. N. van den Pol,et al.  Distribution of metabotropic glutamate receptor mGluR5 immunoreactivity in rat brain , 1995, The Journal of comparative neurology.

[305]  S. Nakanishi,et al.  Analysis of agonist and antagonist activities of phenylglycine derivatives for different cloned metabotropic glutamate receptor subtypes , 1994, The Journal of neuroscience : the official journal of the Society for Neuroscience.

[306]  R. Roth,et al.  Preferential activation of dopamine overflow in prefrontal cortex produced by chronic clozapine treatment , 1994, Neuroscience Letters.

[307]  S. Nakanishi,et al.  Role of the large extracellular domain of metabotropic glutamate receptors in agonist selectivity determination. , 1993, The Journal of biological chemistry.

[308]  P. Chan,et al.  Blockade of glutamate excitotoxicity and its clinical applications , 1993, Neurochemical Research.

[309]  R. Huganir,et al.  Cellular localization of a metabotropic glutamate receptor in rat brain , 1992, Neuron.

[310]  Ben A. Oostra,et al.  Absence of expression of the FMR-1 gene in fragile X syndrome , 1991, Cell.

[311]  F. Ehlert,et al.  Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods. , 1988, Molecular pharmacology.

[312]  W. Poewe,et al.  Low‐dose L‐dopa therapy in Parkinson's disease , 1986, Neurology.

[313]  J. Black,et al.  Operational models of pharmacological agonism , 1983, Proceedings of the Royal Society of London. Series B. Biological Sciences.

[314]  M. E. Goldberg,et al.  Novel non-benzodiazepine anxiolytics , 1983, Neuropharmacology.

[315]  N. Birdsall,et al.  Modification of the binding properties of muscarinic receptors by gallamine. , 1983, Molecular pharmacology.

[316]  J. Patel,et al.  Differential antagonism of the anticonflict effects of typical and atypical anxiolytics. , 1982, European journal of pharmacology.

[317]  J. Pecknold,et al.  Treatment of anxiety using fenobam (a nonbenzodiazepine) in a double-blind standard (diazepam) placebo-controlled study. , 1982, Journal of clinical psychopharmacology.

[318]  S. Stahl,et al.  Building a better antipsychotic: Receptor targets for the treatment of multiple symptom dimensions of schizophrenia , 2011, Neurotherapeutics.

[319]  Amit Etkin,et al.  Functional neuroanatomy of anxiety: a neural circuit perspective. , 2010, Current topics in behavioral neurosciences.

[320]  Craig W Lindsley,et al.  Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia. , 2009, Trends in pharmacological sciences.

[321]  M. Bear,et al.  Fragile X: Translation in Action , 2008, Neuropsychopharmacology.

[322]  S. Lazareno,et al.  Thiochrome enhances acetylcholine affinity at muscarinic M4 receptors: receptor subtype selectivity via cooperativity rather than affinity. , 2004, Molecular pharmacology.

[323]  A. Megens,et al.  Effects of mGlu1 receptor blockade on anxiety-related behaviour in the rat lick suppression test , 2004, Psychopharmacology.

[324]  F. Gasparini,et al.  Neuroprotective activity of metabotropic glutamate receptor ligands. , 2002, Advances in experimental medicine and biology.

[325]  B. Moghaddam,et al.  Distinct contributions of glutamate and dopamine receptors to temporal aspects of rodent working memory using a clinically relevant task , 2001, Psychopharmacology.

[326]  H. Kimelberg,et al.  Metabotropic glutamate receptors in acutely isolated hippocampal astrocytes: Developmental changes of mGluR5 mRNA and functional expression , 2000, Glia.

[327]  W. Drevets Functional anatomical abnormalities in limbic and prefrontal cortical structures in major depression. , 2000, Progress in brain research.

[328]  J. Pin,et al.  Three‐dimensional model of the extracellular domain of the type 4a metabotropic glutamate receptor: New insights into the activation process , 2000, Protein science : a publication of the Protein Society.

[329]  A. Araque,et al.  Astrocyte-induced modulation of synaptic transmission. , 1999, Canadian journal of physiology and pharmacology.

[330]  W. Abraham,et al.  Priming of long‐term potentiation induced by activation of metabotropic glutamate receptors coupled to phospholipase C , 1998, Hippocampus.

[331]  J. Pin,et al.  Pharmacology and functions of metabotropic glutamate receptors. , 1997, Annual review of pharmacology and toxicology.

[332]  J. Ballesteros,et al.  [19] Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors , 1995 .

[333]  D. Jane,et al.  Analysis of Derivatives Subtypes Agonist and Antagonist Activities of Phenylglycine for Different Cloned Metabotropic Glutamate Receptor , 1994 .

[334]  E. Hollander,et al.  Preferential activation of cortical dopamine neurotransmission by clozapine: functional significance. , 1994 .

[335]  W. Poewe,et al.  Treatment of motor fluctuations in Parkinson's disease with an oral sustained-release preparation of L-dopa: clinical and pharmacokinetic observations. , 1986, Clinical neuropharmacology.