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List of works by P. Jeffrey Conn

"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology

scientific article published on 04 March 2011

(3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction

scientific article

3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats

scientific article

3D-QSAR CoMFA study of benzoxazepine derivatives as mGluR5 positive allosteric modulators

scientific article published on 30 July 2010

43.1 GENETIC INSIGHTS LEAD TO DISCOVERY OF SELECTIVE ACTIVATORS OF MGLU1 AND MGLU3 METABOTROPIC GLUTAMATE RECEPTORS AS POTENTIAL TREATMENTS FOR SCHIZOPHRENIA.

scientific article

A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist Flutamide and Its Pharmacologically Active Metabolite 2-Hydroxy-Flutamide as Heterotropic Activators of Cytochrome P450 3A In Vitro and In Vivo

scientific article published on 11 August 2015

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

scientific article published on 9 September 2005

A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.

scientific article

A novel M1 PAM VU0486846 exerts efficacy in cognition models without displaying agonist activity or cholinergic toxicity

scientific article published on 27 April 2018

A novel assay of Gi/o-linked G protein-coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors

scientific article published on 2 January 2008

A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin

scientific article published on 3 May 2009

A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators

scientific article

A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors

scientific article

A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors

scientific article

A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain

scientific article

A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning

scientific article

A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models

scientific article

A rodent model of traumatic stress induces lasting sleep and quantitative electroencephalographic disturbances

scientific article

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

scientific article

A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning

scientific article

A selective positive allosteric modulator of metabotropic glutamate receptor subtype 2 blocks a hallucinogenic drug model of psychosis

scientific article

Activation of M1 and M4 muscarinic receptors as potential treatments for Alzheimer's disease and schizophrenia

scientific article published on 28 January 2014

Activation of Metabotropic Glutamate Receptor 7 Is Required for Induction of Long-Term Potentiation at SC-CA1 Synapses in the Hippocampus

scientific article published on May 2015

Activation of N-methyl-D-aspartate receptors reverses desensitization of metabotropic glutamate receptor, mGluR5, in native and recombinant systems

scientific article

Activation of NMDA receptors reverses desensitization of mGluR5 in native and recombinant systems

scientific article published in March 1999

Activation of group I metabotropic glutamate receptors produces a direct excitation and disinhibition of GABAergic projection neurons in the substantia nigra pars reticulata.

scientific article

Activation of group II metabotropic glutamate receptors induces long-term depression of excitatory synaptic transmission in the substantia nigra pars reticulata

scientific article published on 16 September 2011

Activation of group II metabotropic glutamate receptors inhibits synaptic excitation of the substantia Nigra pars reticulata

scientific article published on 01 May 2000

Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia

scientific article published on 06 December 2008

Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators

scientific article published on 9 October 2015

Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders

scientific article published on May 2017

Allosteric activators of muscarinic receptors as novel approaches for treatment of CNS disorders

scientific article

Allosteric modulation of group III metabotropic glutamate receptor 4: A potential approach to Parkinson's disease treatment ⬇️

scientific article published on October 30, 2003

Allosteric modulation of metabotropic glutamate receptors

scientific article

Allosteric modulation of metabotropic glutamate receptors: structural insights and therapeutic potential

scientific article published on 14 July 2010

Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery

scientific article

Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks

scientific article published on January 2013

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

scientific article published on January 2009

Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells

scientific article

Allosteric potentiators of metabotropic glutamate receptor subtype 5 have differential effects on different signaling pathways in cortical astrocytes

scientific article published on 31 August 2005

An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission

scientific article

An mGlu5-Positive Allosteric Modulator Rescues the Neuroplasticity Deficits in a Genetic Model of NMDA Receptor Hypofunction in Schizophrenia

scientific article published on 7 January 2016

Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100

scientific article

Antipsychotic-like Effects of M4 Positive Allosteric Modulators Are Mediated by CB2 Receptor-Dependent Inhibition of Dopamine Release

scientific article published on 3 September 2016

Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4)

scientific article published on 15 April 2015

Attenuation of cocaine's reinforcing and discriminative stimulus effects via muscarinic M1 acetylcholine receptor stimulation.

scientific article

Biased M1 receptor-positive allosteric modulators reveal role of phospholipase D in M1-dependent rodent cortical plasticity

scientific article published on 03 December 2019

Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery

scientific article published on 5 July 2016

Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents

scientific article

Biotransformation of a novel positive allosteric modulator of metabotropic glutamate receptor subtype 5 contributes to seizure-like adverse events in rats involving a receptor agonism-dependent mechanism

scientific article published on 02 July 2013

Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice

scientific article

Bringing together the academic drug discovery community

scientific article

Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats

scientific article

Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs

scientific article

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides

scientific article published on 6 May 2017

Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.

scientific article published on 3 December 2006

Chemical Modification of the M1 Agonist VU0364572 Reveals Molecular Switches in Pharmacology and a Bitopic Binding Mode ⬇️

scientific article published on September 9, 2012

Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.

scientific article

Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM

scientific article

Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics

scientific article

Cholinergic Projections to the Substantia Nigra Pars Reticulata Inhibit Dopamine Modulation of Basal Ganglia through the M4 Muscarinic Receptor

scientific article published in December 2017

Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators

scientific article published on 26 April 2016

Clozapine potentiation of N-methyl-D-aspartate receptor currents in the nucleus accumbens: role of NR2B and protein kinase A/Src kinases

scientific article published on 19 January 2005

Co-Activation of Metabotropic Glutamate Receptor 3 and Beta-Adrenergic Receptors Modulates Cyclic-AMP, Long-Term Potentiation, and Disrupts Memory Reconsolidation

scientific article

Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7

scientific article

Contextual Fear Extinction Induces Hippocampal Metaplasticity Mediated by Metabotropic Glutamate Receptor 5.

scientific article published on 9 November 2017

Continued optimization of the M5 NAM ML375: Discovery of VU6008667, an M5 NAM with high CNS penetration and a desired short half-life in rat for addiction studies

scientific article published on 13 February 2017

Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor ⬇️

scientific article published on March 29, 2012

Contribution of both M1 and M4 receptors to muscarinic agonist-mediated attenuation of the cocaine discriminative stimulus in mice ⬇️

scientific article published on October 1, 2011

Design and Synthesis of N-Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs

scientific article

Design and Synthesis of an Orally Active Metabotropic Glutamate Receptor Subtype-2 (mGluR2) Positive Allosteric Modulator (PAM) That Decreases Cocaine Self-Administration in Rats ⬇️

scientific article published on December 14, 2010

Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core

scientific article

Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 ⬇️

scientific article published on December 28, 2010

Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence

scientific article

Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2.

scientific article published on 2 November 2015

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

scientific article published on 01 August 2006

Development and Antiparkinsonian Activity of VU0418506, a Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4 Homomers without Activity at mGlu2/4 Heteromers

scientific article

Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type

scientific article published in October 2015

Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380)

scientific article (publication date: 25 September 2014)

Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.

scientific article

Development of a more highly selective M1 antagonist from the continued optimization of the MLPCN Probe ML012 ⬇️

scientific article published on December 6, 2011

Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.

scientific article published on 30 April 2012

Development of a scintillation proximity assay for analysis of Na+/Cl- -dependent neurotransmitter transporter activity

scientific article published on October 2003

Development of allosteric modulators of GPCRs for treatment of CNS disorders

scientific article

Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012 ⬇️

scientific article published on June 15, 2012

Difference in mGluR5 interaction between positive allosteric modulators from two structural classes

scientific article published in November 2003

Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators

scientific article published on 15 March 2018

Differential effects of allosteric M(1) muscarinic acetylcholine receptor agonists on receptor activation, arrestin 3 recruitment, and receptor downregulation

scientific article published on August 2010

Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor

scientific article published on 04 September 2013

Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.

scientific article published on 9 October 2009

Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency

scientific article

Discovery and SAR of a novel series of non-MPEP site mGlu5 PAMs based on an aryl glycine sulfonamide scaffold ⬇️

scientific article published on October 23, 2012

Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition

scientific article published on 21 July 2016

Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators

scientific article

Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype

scientific article published on 03 May 2009

Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).

scientific article

Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4).

scientific article published on 11 May 2016

Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity

scientific article

Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system

scientific article published on January 2010

Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe

scientific article published on January 2009

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core

scientific article published on 05 May 2016

Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): The development of ML169, an MLPCN probe ⬇️

scientific article published on December 9, 2010

Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM)

scientific article

Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound

scientific article

Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy

scientific article published on 19 April 2016

Discovery of ML326: The first sub-micromolar, selective M5 PAM

scientific article

Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor

scientific article published on 6 June 2012

Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation

scientific article

Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity

scientific article published on 13 August 2010

Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety

scientific article published on 10 September 2013

Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia

scientific article published on 20 May 2015

Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety

scientific article published on 11 June 2014

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia

scientific article

Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines

scientific article published in September 2017

Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology

scientific article

Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents

scientific article published on 3 September 2015

Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping

scientific article published on 9 October 2017

Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core

scientific article published on 20 August 2017

Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: Development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia ⬇️

scientific article published on January 1, 2013

Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

scientific article published on 20 September 2017

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

scientific article

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 ⬇️

scientific article published on 03 December 2010

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

scientific article

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

scientific article

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375)

scientific article

Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins

scientific article (publication date: 11 June 2009)

Discovery, Synthesis, and Preclinical Characterization of N-(3-Chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506), a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu4).

scientific article

Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.

scientific article

Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe

scientific article (publication date: August 2014)

Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats

scientific article

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 recept

scientific article published on 19 October 2011

Disease-Modifying Effects of M1 Muscarinic Acetylcholine Receptor Activation in an Alzheimer's Disease Mouse Model

scientific article published on 23 February 2017

Distinct functional roles of the metabotropic glutamate receptors 1 and 5 in the rat globus pallidus

scientific journal article

Distinct physiological roles of the Gq-coupled metabotropic glutamate receptors Co-expressed in the same neuronal populations

scientific article

Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs

scientific article published on 21 December 2016

Dopamine modulates the function of group II and group III metabotropic glutamate receptors in the substantia nigra pars reticulata

scientific article

Effects of VU0410120, a novel GlyT1 inhibitor, on measures of sociability, cognition and stereotypic behaviors in a mouse model of autism

scientific article published on 14 March 2015

Effects of typical and atypical antipsychotics on human glycine transporters

scientific article published in November 2004

Emerging approaches for treatment of schizophrenia: modulation of cholinergic signaling ⬇️

scientific article published on December 1, 2012

Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolin

scientific article

Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function.

scientific article published on 21 October 2011

Functional selectivity induced by mGlu₄ receptor positive allosteric modulation and concomitant activation of Gq coupled receptors

scientific article

Further exploration of M1 allosteric agonists: Subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism ⬇️

scientific article published on November 9, 2012

Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration

scientific article published on 29 April 2016

Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges

scientific article published on 13 December 2014

Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound

scientific article published on 4 July 2015

Glutamate receptors and Parkinson's disease: opportunities for intervention

scientific article

Glutamate receptors as therapeutic targets for Parkinson's disease

scientific article published on December 2009

Group III mGluR regulation of synaptic transmission at the SC-CA1 synapse is developmentally regulated

scientific article published on 24 December 2007

Group III metabotropic glutamate receptor-mediated modulation of the striatopallidal synapse.

scientific article published on August 2003

Group III metabotropic glutamate-receptor-mediated modulation of excitatory transmission in rodent substantia nigra pars compacta dopamine neurons

scientific article

Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators

scientific article

Heterotropic activation of the midazolam hydroxylase activity of CYP3A by a positive allosteric modulator of mGlu5: in vitro to in vivo translation and potential impact on clinically relevant drug-drug interactions

scientific article published on 03 September 2013

Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening

scientific article

Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7

scientific article

Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site

scientific article published on 26 February 2014

Impact of isoflurane anesthesia on D2 receptor occupancy by [18F]fallypride measured by microPET with a modified Logan plot.

scientific article published on 17 June 2011

Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses.

scientific article published on 15 February 2007

Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships

scientific article

Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule

scientific article

Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators

scientific article

Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool

scientific article published on 2 January 2016

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core

scientific article published on 09 October 2015

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs

scientific article published on 10 March 2016

Leveraging bias to your advantage

scientific article published on 01 March 2020

Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes

scientific article

M-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition

M1 muscarinic activation induces long-lasting increase in intrinsic excitability of striatal projection neurons

scientific article published on 20 March 2017

M4 Muscarinic Receptor Signaling Ameliorates Striatal Plasticity Deficits in Models of L-DOPA-Induced Dyskinesia

scientific article published on November 2015

M4 Muscarinic Receptor Signaling Ameliorates Striatal Plasticity Deficits in Models of L-DOPA-Induced Dyskinesia

article by Weixing Shen et al published 1 June 2016 in Neuron

M4 mAChR-mediated modulation of glutamatergic transmission at corticostriatal synapses

scientific article

M5 receptor activation produces opposing physiological outcomes in dopamine neurons depending on the receptor's location

scientific article published on February 2014

MAOS ls for the general synthesis and lead optimization of 3,6-disubstituted-[1,2,4]triazolo[4,3-b]pyridazines

scientific article

MGluR5 mediates the interaction between late-LTP, network activity, and learning

scientific article

Mechanisms underlying prelimbic prefrontal cortex mGlu/mGlu-dependent plasticity and reversal learning deficits following acute stress

article

Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus

scientific journal article

Metabotropic glutamate receptor 3 activation is required for long-term depression in medial prefrontal cortex and fear extinction

scientific article

Metabotropic glutamate receptor subtype 3 gates acute stress-induced dysregulation of amygdalo-cortical function

scientific article published on 21 December 2017

Metabotropic glutamate receptors 1 and 5 differentially regulate CA1 pyramidal cell function.

scientific article

Metabotropic glutamate receptors as therapeutic targets for schizophrenia ⬇️

scientific article published on May 19, 2011

Metabotropic glutamate receptors in the basal ganglia motor circuit

scientific article

Metabotropic glutamate receptors mGluR4 and mGluR8 regulate transmission in the lateral olfactory tract-piriform cortex synapse.

scientific article published on 29 June 2008

Metabotropic glutamate receptors: physiology, pharmacology, and disease

scientific article published on January 2010

Metabotropic glutamate subtype 5 receptors modulate locomotor activity and sensorimotor gating in rodents

scientific article published on 26 March 2003

Modeling Intrahippocampal Effects of Anterior Hippocampal Hyperactivity Relevant to Schizophrenia Using Chemogenetic Excitation of Long Axis–Projecting Mossy Cells in the Mouse Dentate Gyrus

scientific article published in 2021

Modulation of excitatory transmission onto midbrain dopaminergic neurons of the rat by activation of group III metabotropic glutamate receptors

scientific article published in November 2003

Modulation of inhibitory transmission in the rat globus pallidus by activation of mGluR4.

scientific article

Modulation of pyramidal cell output in the medial prefrontal cortex by mGluR5 interacting with CB1 ⬇️

scientific article published on April 6, 2012

Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation

scientific article

Molecular determinants of metabotropic glutamate receptor signaling.

scientific article

Mutual activation of glutamatergic mGlu4 and muscarinic M4 receptors reverses schizophrenia-related changes in rodents

scientific article published on 27 July 2018

N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats

scientific article

N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents

scientific article

N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl- d -aspartate receptor activity ⬇️

scientific article published on October 31, 2003

Neurobiological Insights from mGlu Receptor Allosteric Modulation

scientific article

New therapeutic frontiers for metabotropic glutamate receptors

scientific article

Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: development of a potent and CNS penetrant [3.1.0]-based lead

scientific article

Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: development of a [3.3.0]-based series and other piperidine bioisosteres

scientific article published on 13 January 2014

Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models

scientific article

Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats.

scientific article published on October 2008

Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1.

scientific article published on 23 July 2013

Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders

scientific article

Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology

scientific article published on 13 April 2017

Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover

scientific article published on 24 August 2012

Orally Active Metabotropic Glutamate Subtype 2 Receptor Positive Allosteric Modulators: Structure–Activity Relationships and Assessment in a Rat Model of Nicotine Dependence ⬇️

scientific article published on October 23, 2012

Orthosteric- and allosteric-induced ligand-directed trafficking at GPCRs ⬇️

scientific article published on September 1, 2010

PF-06827443 Displays Robust Allosteric Agonist and Positive Allosteric Modulator Activity in High Receptor Reserve and Native Systems

scientific article published on 23 April 2018

Partial mGlu₅ Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects

scientific article

Pharmacological stimulation of metabotropic glutamate receptor type 4 in a rat model of Parkinson's disease and L-DOPA-induced dyskinesia: Comparison between a positive allosteric modulator and an orthosteric agonist

scientific article published on 4 March 2015

Pharmacology and expression analysis of glycine transporter GlyT1 with [3H]-(N-[3-(4'-fluorophenyl)-3-(4'phenylphenoxy)propyl])sarcosine

scientific article

Pick Your Model Wisely: Understanding the Negative Symptoms of Schizophrenia in Rodent Models

article

Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead

scientific article

Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators

scientific article

Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series

scientific article published on 20 April 2011

Potentiating mGluR5 function with a positive allosteric modulator enhances adaptive learning

scientific article published on 18 July 2013

Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors

scientific article published on 16 February 2016

Preclinical drug discovery research and training at Vanderbilt

scientific article published on 01 January 2007

Prefrontal Cortex-Mediated Impairments in a Genetic Model of NMDA Receptor Hypofunction Are Reversed by the Novel M1 PAM VU6004256.

scientific article published on 12 September 2016

Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia

scientific article published on 28 November 2015

Probing the metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacology

scientific article published on 26 February 2013

Promise of mGluR2/3 activators in psychiatry

scientific article

RGS4 Inhibits Signaling by Group I Metabotropic Glutamate Receptors ⬇️

scientific article published on February 1, 1998

Re-exploration of the PHCCC Scaffold: Discovery of Improved Positive Allosteric Modulators of mGluR4

scientific article

Re-exploration of the mGlu₁ PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR.

scientific article published on 14 March 2016

Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles

scientific article

Role of mGlu5 Receptors and Inhibitory Neurotransmission in M1 Dependent Muscarinic LTD in the Prefrontal Cortex: Implications in Schizophrenia

scientific article published on 5 July 2017

Roles of the M1 muscarinic acetylcholine receptor subtype in the regulation of basal ganglia function and implications for the treatment of Parkinson's disease.

scientific article published on December 2011

Schizophrenia: moving beyond monoamine antagonists

scientific article published on April 2008

Selective actions of novel allosteric modulators reveal functional heteromers of metabotropic glutamate receptors in the CNS

scientific article

Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents

scientific article

Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu₄.

scientific article

Species-Specific Involvement of Aldehyde Oxidase and Xanthine Oxidase in the Metabolism of the Pyrimidine-Containing mGlu5-Negative Allosteric Modulator VU0424238 (Auglurant).

scientific article

Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule

scientific article

State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 - Relation to antipsychotic-like drug effects

scientific article published on 23 November 2015

Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator

scientific article

Structure-Activity Relationships of Pan-Gα Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators

Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonist

scientific article

Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5

scientific article

Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes

scientific article

Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction

scientific article

Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders

scientific article

Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists

scientific article

Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold

scientific article

Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4).

scientific article published on 18 July 2009

Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen

scientific article

Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties

scientific article

Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold ⬇️

scientific article published on January 18, 2011

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).

scientific article

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

scientific article published on 28 October 2009

Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists

scientific article

Synthesis and SAR of substituted pyrazolo[1,5-a]quinazolines as dual mGlu(2)/mGlu(3) NAMs

scientific article published on 20 April 2014

Synthesis and biological characterization of a series of novel diaryl amide M1 antagonists ⬇️

scientific article published on September 23, 2012

Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype

scientific article

Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs)

scientific article

Synthesis and structure-activity relationships of allosteric potentiators of the m(4) muscarinic acetylcholine receptor

scientific article published on October 2009

Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273

scientific article

T227. THE METABOTROPIC GLUTAMATE RECEPTOR SUBTYPE 1 REGULATES STRIATAL DOPAMINE RELEASE VIA AN ENDOCANNABINOID-DEPENDENT MECHANISM: IMPLICATIONS FOR THE TREATMENT OF SCHIZOPHRENIA.

scientific article published in April 2018

Tackling reproducibility in academic preclinical drug discovery

scientific article published on 21 September 2015

Targeting glutamate synapses in schizophrenia ⬇️

scientific article published on September 28, 2011

Targeting metabotropic glutamate receptors for novel treatments of schizophrenia

scientific article

Targeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169.

scientific article

Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅).

scientific article

The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease.

scientific article

The Role of mGlu Receptors in Hippocampal Plasticity Deficits in Neurological and Psychiatric Disorders: Implications for Allosteric Modulators as Novel Therapeutic Strategies

scientific article published on January 2016

The antipsychotic potential of muscarinic allosteric modulation

scientific article

The glycine transporter type 1 inhibitor N-[3-(4'-fluorophenyl)-3-(4'-phenylphenoxy)propyl]sarcosine potentiates NMDA receptor-mediated responses in vivo and produces an antipsychotic profile in rodent behavior.

scientific article published on August 2003

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

scientific article

The mGluR5 antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) potentiates PCP-induced cognitive deficits in rats

scientific article published in September 2004

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.

scientific article

The metabotropic glutamate receptor 8 agonist (S)-3,4-DCPG reverses motor deficits in prolonged but not acute models of Parkinson's disease.

scientific article

The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.

scientific article

Therapeutic Potential of Targeting Metabotropic Glutamate Receptors for Parkinson’s Disease ⬇️

scientific article published on April 1, 2012

Total RNA Sequencing of Rett Syndrome Autopsy Samples Identifies the M4 Muscarinic Receptor as a Novel Therapeutic Target

scientific article published on 9 March 2018

Towards the treatment of Alzheimer's disease: Discovery and development of novel subtype-specific M1 allosteric agonists

article

Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity

scientific article

VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy

scientific article

[(18)F]Fallypride dopamine D2 receptor studies using delayed microPET scans and a modified Logan plot

scientific article published on 03 October 2009

mGlu1 and mGlu5 modulate distinct excitatory inputs to the nucleus accumbens shell

scientific article published on 27 March 2018

mGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndrome

scientific article

mGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome.

scientific article published in August 2017

mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning

scientific article

mGluR7's lucky number

scientific article

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