P. jeffrey Conn

Q: What Schools Are Affiliated With P. jeffrey Conn

P. jeffrey Conn is affiliated with the following schools: Emory University, Vanderbilt University, United States Military Academy

P. jeffrey Conn's AcademicInfluence.com Rankings

P. jeffrey Conn

Medical

#1299

World Rank

#1625

Historical Rank

Pharmacology

#95

World Rank

#123

Historical Rank

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P. jeffrey Conn's Degrees

PhD Pharmacology Vanderbilt University
Bachelors Pharmacy University of Kentucky

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P. jeffrey Conn's Published Works

Number of citations in a given year to any of this author's works

Total number of citations to an author for the works they published in a given year. This highlights publication of the most important work(s) by the author

Published Works

Pharmacology and functions of metabotropic glutamate receptors. (1997) (3105)
Metabotropic glutamate receptors: physiology, pharmacology, and disease. (2010) (1547)
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders (2009) (957)
Metabotropic glutamate receptors in brain function and pathology. (1993) (805)
Metabotropic glutamate receptors: From the workbench to the bedside (2011) (562)
Metabotropic Glutamate Receptors 1 and 5 Differentially Regulate CA1 Pyramidal Cell Function (2001) (437)
Activation of Metabotropic Glutamate Receptor 5 Has Direct Excitatory Effects and Potentiates NMDA Receptor Currents in Neurons of the Subthalamic Nucleus (2000) (415)
Multiple presynaptic metabotropic glutamate receptors modulate excitatory and inhibitory synaptic transmission in hippocampal area CA1 (1995) (369)
Molecular determinants of metabotropic glutamate receptor signaling. (2001) (312)
Metabotropic glutamate receptors in the basal ganglia motor circuit (2005) (305)
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) (293)
N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-d-aspartate receptor activity (2003) (277)
Activation of the genetically defined m1 muscarinic receptor potentiates N-methyl-D-aspartate (NMDA) receptor currents in hippocampal pyramidal cells. (1998) (272)
A unique serotonin receptor in choroid plexus is linked to phosphatidylinositol turnover. (1986) (266)
Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders. (2009) (263)
Allosteric modulation of group III metabotropic glutamate receptor 4: A potential approach to Parkinson's disease treatment (2003) (238)
Novel Selective Allosteric Activator of the M1 Muscarinic Acetylcholine Receptor Regulates Amyloid Processing and Produces Antipsychotic-Like Activity in Rats (2008) (228)
Relative efficacies of piperazines at the phosphoinositide hydrolysis-linked serotonergic (5-HT-2 and 5-HT-1c) receptors. (1987) (225)
Glutamate receptors as therapeutic targets for Parkinson's disease. (2009) (224)
A Selective Allosteric Potentiator of the M1 Muscarinic Acetylcholine Receptor Increases Activity of Medial Prefrontal Cortical Neurons and Restores Impairments in Reversal Learning (2009) (221)
Metabotropic Glutamate Subtype 5 Receptors Modulate Locomotor Activity and Sensorimotor Gating in Rodents (2003) (218)
Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders (2014) (213)
A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. (2003) (209)
Immunocytochemical localization of group III metabotropic glutamate receptors in the hippocampus with subtype-specific antibodies (1996) (209)
Development of allosteric modulators of GPCRs for treatment of CNS disorders (2014) (204)
Serotonin-stimulated phosphoinositide turnover: mediation by the S2 binding site in rat cerebral cortex but not in subcortical regions. (1985) (204)
The contribution of protease-activated receptor 1 to neuronal damage caused by transient focal cerebral ischemia (2003) (202)
mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning (2009) (200)
Activation of NMDA receptors reverses desensitization of mGluR5 in native and recombinant systems (1999) (199)
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery. (2012) (196)
Regulation of serotonin-stimulated phosphoinositide hydrolysis: relation to the serotonin 5-HT-2 binding site (1986) (194)
Tyrosine kinase potentiates NMDA receptor currents by reducing tonic zinc inhibition (1998) (189)
Discovery, Characterization, and Antiparkinsonian Effect of Novel Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4 (2008) (189)
Excitatory effects of ACPD receptor activation in the hippocampus are mediated by direct effects on pyramidal cells and blockade of synaptic inhibition. (1991) (186)
Centrally Active Allosteric Potentiators of the M4 Muscarinic Acetylcholine Receptor Reverse Amphetamine-Induced Hyperlocomotor Activity in Rats (2008) (182)
Differential involvement of group II and group III mGluRs as autoreceptors at lateral and medial perforant path synapses. (1996) (180)
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 (2003) (176)
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) (174)
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) (171)
Selective 5ht-2 antagonists inhibit serotonin stimulated phosphatidylinositol metabolism in cerebral cortex (1984) (171)
Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders (2017) (170)
A Novel Selective Allosteric Modulator Potentiates the Activity of Native Metabotropic Glutamate Receptor Subtype 5 in Rat Forebrain (2004) (170)
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) (170)
Biphenyl-indanone A, a Positive Allosteric Modulator of the Metabotropic Glutamate Receptor Subtype 2, Has Antipsychotic- and Anxiolytic-Like Effects in Mice (2006) (169)
Distribution and roles of metabotropic glutamate receptors in the basal ganglia motor circuit: implications for treatment of Parkinson's disease and related disorders. (2000) (166)
Immunohistochemical localization of subtype 4a metabotropic glutamate receptors in the rat and mouse basal ganglia (1999) (166)
Roles of specific metabotropic glutamate receptor subtypes in regulation of hippocampal CA1 pyramidal cell excitability. (1995) (165)
Group III Metabotropic Glutamate Receptor-Mediated Modulation of the Striatopallidal Synapse (2003) (165)
Localization of metabotropic glutamate receptor 7 mRNA and mGluR7a protein in the rat basal ganglia (1999) (164)
"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology. (2011) (157)
A Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 2 Blocks a Hallucinogenic Drug Model of Psychosis (2007) (154)
M4 Muscarinic Receptor Signaling Ameliorates Striatal Plasticity Deficits in Models of L-DOPA-Induced Dyskinesia (2015) (149)
RGS4 Inhibits Signaling by Group I Metabotropic Glutamate Receptors (1998) (147)
An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission. (2008) (143)
Activation of Group II Metabotropic Glutamate Receptors Inhibits Synaptic Excitation of the Substantia Nigra Pars Reticulata (2000) (138)
Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors. (2016) (137)
Discovery and Characterization of Novel Allosteric Potentiators of M1 Muscarinic Receptors Reveals Multiple Modes of Activity (2009) (136)
Direct and indirect modulation of the N-methyl D-aspartate receptor. (2002) (133)
Protein Kinase C and A3 Adenosine Receptor Activation Inhibit Presynaptic Metabotropic Glutamate Receptor (mGluR) Function and Uncouple mGluRs from GTP-Binding Proteins (1998) (129)
Activation of Group I Metabotropic Glutamate Receptors Produces a Direct Excitation and Disinhibition of GABAergic Projection Neurons in the Substantia Nigra Pars Reticulata (2001) (128)
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. (2006) (123)
Distinct physiological roles of the Gq‐coupled metabotropic glutamate receptors co‐expressed in the same neuronal populations (2002) (122)
Allosteric interaction between the amino terminal domain and the ligand binding domain of NR2A (2001) (122)
The mGluR5 antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) potentiates PCP-induced cognitive deficits in rats (2004) (121)
Activation of metabotropic glutamate receptors increases cAMP accumulation in hippocampus by potentiating responses to endogenous adenosine (1993) (120)
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) (119)
Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes (2015) (118)
Allosteric modulation of metabotropic glutamate receptors: Structural insights and therapeutic potential (2011) (118)
A Novel Selective Muscarinic Acetylcholine Receptor Subtype 1 Antagonist Reduces Seizures without Impairing Hippocampus-Dependent Learning (2009) (117)
Functional Impact of Allosteric Agonist Activity of Selective Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 in Regulating Central Nervous System Function (2012) (113)
Allosteric Potentiators of Metabotropic Glutamate Receptor Subtype 5 Have Differential Effects on Different Signaling Pathways in Cortical Astrocytes (2005) (111)
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 (2008) (110)
Glutamate Receptors and Parkinson’s Disease (2003) (107)
Metabotropic Glutamate Receptor 5-Induced Phosphorylation of Extracellular Signal-Regulated Kinase in Astrocytes Depends on Transactivation of the Epidermal Growth Factor Receptor (2001) (105)
Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors. (2006) (104)
Novel Allosteric Agonists of M1 Muscarinic Acetylcholine Receptors Induce Brain Region-Specific Responses That Correspond with Behavioral Effects in Animal Models (2012) (102)
Targeting glutamate synapses in schizophrenia. (2011) (102)
Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents (2015) (102)
Selective Actions of Novel Allosteric Modulators Reveal Functional Heteromers of Metabotropic Glutamate Receptors in the CNS (2014) (101)
Muscarinic receptor subtypes involved in hippocampal circuits. (1999) (100)
Selective Activation of M4 Muscarinic Acetylcholine Receptors Reverses MK-801-Induced Behavioral Impairments and Enhances Associative Learning in Rodents (2014) (100)
Phosphorylation of Mitogen‐Activated Protein Kinase in Cultured Rat Cortical Glia by Stimulation of Metabotropic Glutamate Receptors (1998) (99)
Unique Signaling Profiles of Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Determine Differences in In Vivo Activity (2013) (98)
Selective activation of phosphoinositide hydrolysis by a rigid analogue of glutamate (1990) (96)
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) (96)
Group III Metabotropic Glutamate-Receptor-Mediated Modulation of Excitatory Transmission in Rodent Substantia Nigra Pars Compacta Dopamine Neurons (2005) (95)
Activation of group III mGluRs inhibits GABAergic and glutamatergic transmission in the substantia nigra pars reticulata. (2001) (94)
Antipsychotic-like Effects of M4 Positive Allosteric Modulators Are Mediated by CB2 Receptor-Dependent Inhibition of Dopamine Release (2016) (94)
Metabotropic Excitatory Amino Acid Receptor Activation Stimulates Phospholipase D in Hippocampal Slices (1992) (93)
NMDA-induced potentiation of mGluR5 is mediated by activation of protein phosphatase 2B/calcineurin (2005) (92)
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) (92)
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. (2009) (92)
Down‐Regulation of AMPA Receptor Subunit GluR2 in Amygdaloid Kindling (1995) (90)
Metabotropic glutamate receptors as therapeutic targets for schizophrenia (2012) (89)
Antipsychotic Drug-Like Effects of the Selective M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator VU0152100 (2014) (88)
Distribution and Developmental Regulation of Metabotropic Glutamate Receptor 7a in Rat Brain (1998) (88)
Activation of M1 and M4 muscarinic receptors as potential treatments for Alzheimer’s disease and schizophrenia (2014) (86)
Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M1 receptor function in the central nervous system (2010) (84)
Investigating Metabotropic Glutamate Receptor 5 Allosteric Modulator Cooperativity, Affinity, and Agonism: Enriching Structure-Function Studies and Structure-Activity Relationships (2012) (84)
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) (84)
Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold. (2008) (80)
Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks. (2013) (79)
Metabotropic glutamate receptor 3 activation is required for long-term depression in medial prefrontal cortex and fear extinction (2015) (78)
Distinct Functional Roles of the Metabotropic Glutamate Receptors 1 and 5 in the Rat Globus Pallidus (2003) (78)
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. (2011) (78)
Activation of Metabotropic Glutamate Receptors in the Hippocampus Increases Cyclic AMP Accumulation (1992) (78)
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) (78)
Presynaptic enhancement of excitatory synaptic transmission by beta-adrenergic receptor activation. (1994) (78)
A Novel Family of Potent Negative Allosteric Modulators of Group II Metabotropic Glutamate Receptors (2007) (78)
Context-Dependent Pharmacology Exhibited by Negative Allosteric Modulators of Metabotropic Glutamate Receptor 7 (2010) (77)
M4 mAChR-mediated modulation of glutamatergic transmission at corticostriatal synapses. (2014) (76)
Agonist‐Induced Phosphoinositide Hydrolysis in Choroid Plexus (1986) (76)
Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). (2009) (75)
A Novel Metabotropic Glutamate Receptor 5 Positive Allosteric Modulator Acts at a Unique Site and Confers Stimulus Bias to mGlu5 Signaling (2013) (75)
Group III mGluR regulation of synaptic transmission at the SC-CA1 synapse is developmentally regulated (2008) (75)
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) (74)
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 (2013) (73)
Discovery of a Novel Chemical Class of mGlu5 Allosteric Ligands with Distinct Modes of Pharmacology (2010) (72)
Novel mGluR5 Positive Allosteric Modulator Improves Functional Recovery, Attenuates Neurodegeneration, and Alters Microglial Polarization after Experimental Traumatic Brain Injury (2014) (72)
Opportunities and Challenges of Psychiatric Drug Discovery: Roles for Scientists in Academic, Industry, and Government Settings (2008) (71)
Up‐regulation of the metabotropic glutamate receptor mGluR4 in hippocampal neurons with reduced seizure vulnerability (2000) (71)
NMDA-induced phosphorylation and regulation of mGluR5 (2002) (68)
Heterogeneity of metabotropic glutamate receptors in autonomic cell groups of the medulla oblongata of the rat (1999) (68)
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) (66)
Allosteric modulation of metabotropic glutamate receptors. (2011) (66)
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. (2007) (66)
New therapeutic frontiers for metabotropic glutamate receptors. (2005) (65)
Protein kinase inhibitors selectively block phorbol ester- or forskolin- induced changes in excitability of Aplysia neurons (1989) (65)
cAMP-Dependent Protein Kinase Inhibits mGluR2 Coupling to G-Proteins by Direct Receptor Phosphorylation (2000) (65)
Roles of the M1 Muscarinic Acetylcholine Receptor Subtype in the Regulation of Basal Ganglia Function and Implications for the Treatment of Parkinson's Disease (2012) (64)
Potentiation of M1 Muscarinic Receptor Reverses Plasticity Deficits and Negative and Cognitive Symptoms in a Schizophrenia Mouse Model (2016) (64)
Functional partnership between mGlu3 and mGlu5 metabotropic glutamate receptors in the central nervous system (2018) (63)
M5 Receptor Activation Produces Opposing Physiological Outcomes in Dopamine Neurons Depending on the Receptor's Location (2014) (62)
L-cysteine sulfinic acid as an endogenous agonist of a novel metabotropic receptor coupled to stimulation of phospholipase D activity. (1994) (62)
Multiple metabotropic glutamate receptors regulate hippocampal function (1992) (60)
Emerging approaches for treatment of schizophrenia: modulation of cholinergic signaling. (2012) (60)
Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe. (2011) (59)
Allosteric activators of muscarinic receptors as novel approaches for treatment of CNS disorders. (2010) (58)
Cyclic AMP‐dependent protein kinase phosphorylates group III metabotropic glutamate receptors and inhibits their function as presynaptic receptors (2001) (58)
Pharmacology and expression analysis of glycine transporter GlyT1 with [3H]-(N-[3-(4′-fluorophenyl)-3-(4′phenylphenoxy)propyl])sarcosine (2003) (57)
Tackling reproducibility in academic preclinical drug discovery (2015) (56)
Bringing together the academic drug discovery community (2013) (55)
Inhibitors of protein kinase C prevent enhancement of calcium current and action potentials in peptidergic neurons of Aplysia (1989) (53)
A cyclic AMP-dependent form of associative synaptic plasticity induced by coactivation of beta-adrenergic receptors and metabotropic glutamate receptors in rat hippocampus (1994) (53)
Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus (2005) (53)
Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents. (2015) (53)
Metabotropic Glutamate Receptor (mGluR)‐Mediated Potentiation of Cyclic AMP Responses Does Not Require Phosphoinositide Hydrolysis: Mediation by a Group II‐Like mGluR (1995) (52)
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). (2013) (51)
mGlu2 and mGlu3 Negative Allosteric Modulators Divergently Enhance Thalamocortical Transmission and Exert Rapid Antidepressant-like Effects (2019) (51)
Identification of Positive Allosteric Modulators VU0155094 (ML397) and VU0422288 (ML396) Reveals New Insights into the Biology of Metabotropic Glutamate Receptor 7 (2014) (51)
The antipsychotic potential of muscarinic allosteric modulation. (2010) (51)
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. (2010) (51)
An mGlu5-Positive Allosteric Modulator Rescues the Neuroplasticity Deficits in a Genetic Model of NMDA Receptor Hypofunction in Schizophrenia (2016) (51)
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) (51)
The bag cell neurons ofAplysia (2007) (51)
Selective potentiation of the metabotropic glutamate receptor subtype 2 blocks phencyclidine-induced hyperlocomotion and brain activation (2010) (50)
mGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome (2017) (50)
Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead. (2009) (50)
Denervation supersensitivity of 5-HT-1c receptors in rat choroid plexus (1987) (50)
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). (2013) (49)
Pharmacology and physiology of metabotropic glutamate receptors in mammalian central nervous system (1991) (49)
Dopamine Modulates the Function of Group II and Group III Metabotropic Glutamate Receptors in the Substantia Nigra Pars Reticulata (2002) (48)
Effects of typical and atypical antipsychotics on human glycine transporters (2004) (48)
M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition (2018) (48)
Role for the M1 Muscarinic Acetylcholine Receptor in Top-Down Cognitive Processing Using a Touchscreen Visual Discrimination Task in Mice. (2015) (47)
Clozapine Potentiation of N-Methyl-d-aspartate Receptor Currents in the Nucleus Accumbens: Role of NR2B and Protein Kinase A/Src Kinases (2005) (47)
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. (2008) (47)
Re-exploration of the PHCCC Scaffold: Discovery of Improved Positive Allosteric Modulators of mGluR4. (2010) (46)
Peripheral glutamate receptors: molecular biology and role in taste sensation. (2000) (46)
Development and Antiparkinsonian Activity of VU0418506, a Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4 Homomers without Activity at mGlu2/4 Heteromers. (2016) (44)
N-Aryl Piperazine Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators Possess Efficacy in Preclinical Models of NMDA Hypofunction and Cognitive Enhancement (2013) (44)
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) (44)
Chemical Modulation of Mutant mGlu1 Receptors Derived from Deleterious GRM1 Mutations Found in Schizophrenics (2014) (44)
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 (2013) (43)
Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold. (2011) (43)
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) (43)
Modulation of pyramidal cell output in the medial prefrontal cortex by mGluR5 interacting with CB1 (2013) (43)
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 antagonists. (2009) (43)
Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery (2017) (42)
Attenuation of Cocaine's Reinforcing and Discriminative Stimulus Effects via Muscarinic M1 Acetylcholine Receptor Stimulation (2010) (42)
Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells (2008) (42)
Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site. (2014) (42)
The bag cell neurons of Aplysia. A model for the study of the molecular mechanisms involved in the control of prolonged animal behaviors. (1989) (41)
Cholinergic Projections to the Substantia Nigra Pars Reticulata Inhibit Dopamine Modulation of Basal Ganglia through the M4 Muscarinic Receptor (2017) (41)
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. (2012) (41)
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. (2011) (41)
Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening (2010) (40)
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 (2012) (40)
mGluR7's lucky number. (2006) (40)
Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs. (2017) (39)
Central serotonin receptors: effector systems, physiological roles and regulation (2004) (39)
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 (2015) (39)
Haloperidol-induced alteration in the physiological actions of group I mGlus in the subthalamic nucleus and the substantia nigra pars reticulata (2002) (39)
The Role of Aldehyde Oxidase and Xanthine Oxidase in the Biotransformation of a Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 (2012) (39)
mGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndrome. (2016) (38)
Localization and physiological roles of metabotropic glutamate receptors in the direct and indirect pathways of the basal ganglia (2002) (38)
Promise of mGluR2/3 activators in psychiatry (2009) (38)
Emerging approaches for treatment of schizophrenia: modulation of glutamatergic signaling. (2012) (38)
Biochemical characterization of serotonin stimulated phosphoinositide turnover. (1986) (38)
Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia. (2015) (38)
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. (2014) (37)
Modulation of the basal ganglia by metabotropic glutamate receptors: potential for novel therapeutics. (2002) (37)
Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation (2015) (37)
Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia. (2017) (37)
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) (36)
Amygdala Kindling Alters Protein Kinase C Activity in Dentate Gyrus (1992) (36)
Synthesis, SAR and Unanticipated Pharmacological Profiles of Analogues of the mGluR5 Ago‐potentiator ADX‐47273 (2009) (36)
Allosteric activation of M4 muscarinic receptors improve behavioral and physiological alterations in early symptomatic YAC128 mice (2015) (36)
Activation of groups I or III metabotropic glutamate receptors inhibits excitatory transmission in the rat subthalamic nucleus (2001) (35)
Metabotropic glutamate receptors for new treatments in schizophrenia. (2012) (35)
Relationship between In Vivo Receptor Occupancy and Efficacy of Metabotropic Glutamate Receptor Subtype 5 Allosteric Modulators with Different In Vitro Binding Profiles (2015) (35)
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM. (2012) (35)
Disease-Modifying Effects of M1 Muscarinic Acetylcholine Receptor Activation in an Alzheimer's Disease Mouse Model. (2017) (35)
Activation of Metabotropic Glutamate Receptor 7 Is Required for Induction of Long-Term Potentiation at SC-CA1 Synapses in the Hippocampus (2015) (35)
Effector systems coupled to serotonin receptors in brain: serotonin stimulated phosphoinositide hydrolysis. (1986) (34)
A Novel M1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity. (2018) (34)
Positive allosteric modulation of M1 and M4 muscarinic receptors as potential therapeutic treatments for schizophrenia (2017) (34)
Contribution of both M1 and M4 receptors to muscarinic agonist-mediated attenuation of the cocaine discriminative stimulus in mice (2012) (34)
Discovery of N-Aryl Piperazines as Selective mGluR5 Potentiators with Improved In Vivo Utility (2010) (34)
Immunohistochemical Distribution of RGS7 Protein and Cellular Selectivity in Colocalizing with Gαq Proteins in the Adult Rat Brain (1999) (34)
Group I and group II metabotropic glutamate receptor allosteric modulators as novel potential antipsychotics. (2015) (34)
Potentiating mGluR5 function with a positive allosteric modulator enhances adaptive learning (2013) (34)
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). (2016) (34)
Interaction between metabotropic glutamate receptor 7 and alpha tubulin (2002) (33)
A rodent model of traumatic stress induces lasting sleep and quantitative electroencephalographic disturbances. (2015) (33)
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 (2014) (33)
Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype. (2009) (32)
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties. (2008) (32)
Synthesis and Structure–Activity Relationships of Allosteric Potentiators of the M4 Muscarinic Acetylcholine Receptor (2009) (32)
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071. (2011) (31)
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. (2012) (31)
Dissociation of protein kinase-mediated regulation of metabotropic glutamate receptor 7 (mGluR7) interactions with calmodulin and regulation of mGluR7 function. (2002) (31)
Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system. (2010) (31)
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. (2013) (31)
Differential regulation of metabotropic glutamate receptor 5‐mediated phosphoinositide hydrolysis and extracellular signal‐regulated kinase responses by protein kinase C in cultured astrocytes (2002) (31)
Functional downregulation of GluR2 in piriform cortex of kindled animals (2000) (31)
Design and Synthesis of N-Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs. (2017) (31)
Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4). (2009) (30)
Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core. (2017) (30)
VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy (2016) (30)
Partial mGlu5 Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects (2016) (30)
Cognitive enhancement and antipsychotic-like activity following repeated dosing with the selective M4 PAM VU0467154 (2018) (30)
Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode. (2012) (29)
Orthosteric- and allosteric-induced ligand-directed trafficking at GPCRs. (2010) (29)
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)picolinamide (ML254). (2013) (29)
Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2. (2015) (29)
Activation of group II metabotropic glutamate receptors induces long-term depression of excitatory synaptic transmission in the substantia nigra pars reticulata (2011) (29)
Potentiation of mGlu5 receptors with the novel enhancer, VU0360172, reduces spontaneous absence seizures in WAG/Rij rats (2013) (28)
Therapeutic potential of targeting metabotropic glutamate receptors for Parkinson's disease. (2012) (28)
M1 muscarinic activation induces long-lasting increase in intrinsic excitability of striatal projection neurons (2017) (28)
Activation of PKC Disrupts Presynaptic Inhibition by Group II and Group III Metabotropic Glutamate Receptors and Uncouples the Receptor from GTP‐Binding Proteins (1999) (28)
The Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator ADX88178 Inhibits Inflammatory Responses in Primary Microglia (2016) (28)
Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule. (2013) (27)
Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs. (2017) (27)
Roles of the M4 acetylcholine receptor in the basal ganglia and the treatment of movement disorders (2019) (27)
Pharmacological differentiation of metabotropic glutamate receptors coupled to potentiation of cyclic adenosine monophosphate responses and phosphoinositide hydrolysis. (1993) (27)
[(18)F]Fallypride dopamine D2 receptor studies using delayed microPET scans and a modified Logan plot. (2009) (27)
Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). (2010) (26)
Activation of N‐Methyl‐D‐Aspartate Receptors Reverses Desensitization of Metabotropic Glutamate Receptor, mGluR5, in Native and Recombinant Systems (1999) (26)
Activation of metabotropic glutamate receptor 1 inhibits glutamatergic transmission in the substantia nigra pars reticulata (2001) (26)
The metabotropic glutamate receptor 8 agonist (S)-3,4-DCPG reverses motor deficits in prolonged but not acute models of Parkinson's disease (2013) (26)
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. (2008) (26)
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. (2013) (25)
Metabotropic glutamate receptors modulate feedback inhibition in a developmentally regulated manner in rat dentate gyrus (2004) (25)
Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence. (2012) (25)
Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators. (2010) (25)
mGlu1 and mGlu5 modulate distinct excitatory inputs to the nucleus accumbens shell (2018) (25)
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) (2014) (24)
Discovery, Synthesis and Characterization of a Highly Muscarinic Acetylcholine Receptor (mAChR)‐Selective M5‐Orthosteric Antagonist, VU0488130 (ML381): A Novel Molecular Probe (2014) (24)
Differential effects of allosteric M(1) muscarinic acetylcholine receptor agonists on receptor activation, arrestin 3 recruitment, and receptor downregulation. (2010) (23)
Protein Kinase C and A 3 Adenosine Receptor Activation Inhibit Presynaptic Metabotropic Glutamate Receptor ( mGluR ) Function and Uncouple mGluRs from GTP-Binding Proteins (1998) (23)
Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators. (2016) (23)
Head-to head comparison of mGlu1 and mGlu5 receptor activation in chronic treatment of absence epilepsy in WAG/Rij rats (2014) (23)
Development of a scintillation proximity assay for analysis of Na+/Cl- -dependent neurotransmitter transporter activity. (2003) (23)
Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators (2018) (23)
Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor. (2013) (23)
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 (2017) (22)
Synthesis and SAR of substituted pyrazolo[1,5-a]quinazolines as dual mGlu(2)/mGlu(3) NAMs. (2014) (22)
Total RNA Sequencing of Rett Syndrome Autopsy Samples Identifies the M4 Muscarinic Receptor as a Novel Therapeutic Target (2018) (22)
3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats. (2010) (22)
Extracellular Calcium Modulates Actions of Orthosteric and Allosteric Ligands on Metabotropic Glutamate Receptor 1α* (2013) (21)
Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines. (2017) (21)
4-Methylhomoibotenic acid activates a novel metabotropic glutamate receptor coupled to phosphoinositide hydrolysis. (1997) (21)
Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule. (2013) (21)
Novel Potential Therapeutics for Schizophrenia: Focus on the Modulation of Metabotropic Glutamate Receptor Function (2005) (21)
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. (2010) (21)
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. (2017) (20)
Role of mGlu5 Receptors and Inhibitory Neurotransmission in M1 Dependent Muscarinic LTD in the Prefrontal Cortex: Implications in Schizophrenia. (2017) (20)
Discovery of ML326: The first sub-micromolar, selective M5 PAM. (2013) (20)
Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators (2018) (20)
(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. (2011) (20)
Metabotropic glutamate receptors mGluR4 and mGluR8 regulate transmission in the lateral olfactory tract–piriform cortex synapse (2008) (19)
VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides. (2017) (19)
Effects of VU0410120, a novel GlyT1 inhibitor, on measures of sociability, cognition and stereotypic behaviors in a mouse model of autism (2015) (19)
M4 Muscarinic Receptor Signaling Ameliorates Striatal Plasticity Deficits in Models of L-DOPA-Induced Dyskinesia (2016) (19)
4‐Bromohomoibotenic Acid Selectively Activates a 1‐Aminocyclopentane‐1S,3R‐Dicarboxylic Acid‐Insensitive Metabotropic Glutamate Receptor Coupled to Phosphoinositide Hydrolysis in Rat Cortical Slices (1994) (19)
Species-Specific Involvement of Aldehyde Oxidase and Xanthine Oxidase in the Metabolism of the Pyrimidine-Containing mGlu5-Negative Allosteric Modulator VU0424238 (Auglurant) (2017) (19)
Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962). (2019) (18)
Opportunities and Challenges of Psychiatric Drug Discovery: Roles for Scientists in Academic, Industry, and Government Settings (2008) (18)
Targeting muscarinic receptors to treat schizophrenia (2021) (18)
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 (2013) (18)
State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 – Relation to antipsychotic-like drug effects (2016) (18)
Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4) (2015) (18)
Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS. (2009) (18)
Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. (2009) (17)
Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold. (2012) (17)
Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5. (2010) (17)
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 and Mutant mGlu1 Receptors Found in Schizophrenics (2015) (16)
Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides. (2017) (16)
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. (2016) (16)
Kinetic and system bias as drivers of metabotropic glutamate receptor 5 allosteric modulator pharmacology (2019) (16)
Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges. (2015) (16)
Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor. (2012) (16)
Second-Messenger Systems Coupled to Metabotropic Glutamate Receptors (1994) (16)
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. (2013) (16)
Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor (2018) (16)
Discovery of VU2957 (Valiglurax): An mGlu4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease. (2018) (15)
A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin. (2009) (15)
PF-06827443 Displays Robust Allosteric Agonist and Positive Allosteric Modulator Activity in High Receptor Reserve and Native Systems. (2018) (15)
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists. (2008) (15)
mGluR5 positive allosteric modulators (2008) (15)
Antidepressant potential of metabotropic glutamate receptor mGlu2 and mGlu3 negative allosteric modulators (2018) (14)
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. (2011) (14)
Impact of isoflurane anesthesia on D2 receptor occupancy by [18F]fallypride measured by microPET with a modified Logan plot (2011) (14)
Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series. (2011) (14)
N- -2-hydroxybenzamide (CPPHA) Acts through a Novel Site as a Positive Allosteric Modulator of Group 1 Metabotropic Glutamate Receptors (2007) (14)
Co-Activation of Metabotropic Glutamate Receptor 3 and Beta-Adrenergic Receptors Modulates Cyclic-AMP and Long-Term Potentiation, and Disrupts Memory Reconsolidation (2017) (14)
Metabotropic Glutamate Receptors As Emerging Targets for the Treatment of Schizophrenia (2022) (14)
Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology. (2017) (14)
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. (2016) (13)
Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012. (2012) (13)
Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes. (2016) (13)
Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu4). (2018) (13)
N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. (2013) (13)
Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators (2012) (12)
Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a]pyrimidine-5-carboxamide and Thieno[3,2- b]pyridine-5-carboxamide Cores. (2018) (12)
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core. (2015) (12)
mGlu5 Positive Allosteric Modulators Facilitate Long-Term Potentiation via Disinhibition Mediated by mGlu5-Endocannabinoid Signaling (2019) (12)
Muscarinic receptor M4 positive allosteric modulators attenuate central effects of cocaine. (2017) (12)
MAOS protocols for the general synthesis and lead optimization of 3,6-disubstituted-[1,2,4]triazolo[4,3-b]pyridazines (2009) (12)
Neurobiological Insights from mGlu Receptor Allosteric Modulation (2015) (12)
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. (2009) (12)
Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping. (2017) (11)
Tetrahydronaphthyridine and Dihydronaphthyridinone Ethers As Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 5 (mGlu5) (2014) (11)
A close structural analog of MPEP acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators (2005) (11)
Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover. (2012) (11)
Functional selectivity induced by mGlu4 receptor positive allosteric modulation and concomitant activation of Gq coupled receptors (2013) (11)
Regulation of Neuronal Circuits and Animal Behavior by Metabotropic Glutamate Receptors (1994) (10)
Roles of the M 1 Muscarinic Acetylcholine Receptor Subtype in the Regulation of Basal Ganglia Function and Implications for the Treatment of Parkinson ’ s Disease (2012) (10)
VU6007477, a Novel M1 PAM Based on a Pyrrolo[2,3-b]pyridine Carboxamide Core Devoid of Cholinergic Adverse Events. (2018) (10)
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. (2017) (10)
Modulation of Excitatory Transmission onto Midbrain Dopaminergic Neurons of the Rat by Activation of Group III Metabotropic Glutamate Receptors (2003) (10)
mGlu1 potentiation enhances prelimbic somatostatin interneuron activity to rescue schizophrenia-like physiological and cognitive deficits (2021) (10)
Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition. (2016) (10)
Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration. (2016) (10)
A GRM7 mutation associated with developmental delay reduces mGlu7 expression and produces neurological phenotypes (2021) (10)
Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (2013) (9)
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism. (2013) (9)
The Role of mGlu Receptors in Hippocampal Plasticity Deficits in Neurological and Psychiatric Disorders: Implications for Allosteric Modulators as Novel Therapeutic Strategies (2016) (9)
M1 and M3 muscarinic receptors may play a role in the neurotoxicity of anhydroecgonine methyl ester, a cocaine pyrolysis product (2015) (9)
Input-specific regulation of glutamatergic synaptic transmission in the medial prefrontal cortex by mGlu2/mGlu4 receptor heterodimers (2021) (9)
Modulation of arousal and sleep/wake architecture by M1 PAM VU0453595 across young and aged rodents and nonhuman primates (2020) (9)
Examining the role of muscarinic M5 receptors in VTA cholinergic modulation of depressive-like and anxiety-related behaviors in rats (2020) (9)
The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core. (2018) (9)
Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold. (2018) (9)
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: development of a potent and CNS penetrant [3.1.0]-based lead. (2014) (8)
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 (2015) (8)
Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1. (2013) (8)
Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency. (2014) (8)
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs. (2016) (8)
Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu4 positive allosteric modulators that mitigate CYP1A2 induction liability. (2018) (8)
Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). (2015) (8)
Structure-Activity Relationships of Pan-Gαq/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators. (2018) (8)
Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound. (2015) (8)
Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity (2010) (8)
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. (2016) (8)
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. (2015) (8)
Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists. (2017) (7)
Discovery of a novel 3,4-dimethylcinnoline carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping. (2019) (7)
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. (2016) (7)
Re-exploration of the mGlu₁ PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR. (2016) (7)
Modulation of neuronal microcircuit activities within the medial prefrontal cortex by mGluR5 positive allosteric modulator (2014) (7)
The Metabotropic Glutamate Receptor 4-Positive Allosteric Modulator VU 0364770 Produces Efficacy Alone and in Combination with L-DOPA or an Adenosine 2 A Antagonist in Preclinical Rodent Models of Parkinson ’ s Disease (2012) (7)
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. (2017) (7)
Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity. (2010) (7)
In Vitro to in Vivo Translation of Allosteric Modulator Concentration-Effect Relationships: Implications for Drug Discovery. (2019) (7)
3D-QSAR CoMFA study of benzoxazepine derivatives as mGluR5 positive allosteric modulators. (2010) (6)
The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate. (2019) (6)
Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy. (2021) (5)
Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu7 Positive Allosteric Modulator Tool Compound. (2020) (5)
Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012. (2012) (5)
Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core. (2017) (5)
Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. (2014) (5)
Functional impact of allosteric agonist activity of selective positive allosteric modulators of mGlu 5 in regulating CNS function (2011) (5)
Novel M4 positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands. (2019) (5)
Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators. (2015) (5)
Identification of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Acting at Site Distinct from 2-Methyl-6-(phenylethynyl)-pyridine Binding (2019) (5)
A NOVEL CLASS OF POSITIVE ALLOSTERIC MODULATORS OF mGluR1 INTERACT WITH A SITE DISTINCT FROM THAT OF NEGATIVE ALLOSTERIC MODULATORS (2006) (5)
Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu₄. (2011) (5)
Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists. (2010) (5)
Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4). (2016) (5)
Synthesis and biological characterization of a series of novel diaryl amide M₁ antagonists. (2012) (5)
Metabotropic Glutamate Receptor–Dopamine Interactions in the Basal Ganglia Motor Circuit (2011) (4)
Preclinical drug discovery research and training at Vanderbilt. (2007) (4)
Development of the First Selective mGlu3 NAM from an mGlu5 PAM Hit (2013) (4)
Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M1 Positive Allosteric Modulators. (2018) (4)
Novel PAMs Targeting NMDAR GluN2A Subunit (2016) (4)
Metabotropic Glutamate Receptor Ligands as Novel Therapeutic Agents (2008) (4)
Scheme 1, Reagents and conditions (2013) (4)
Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu2/4 heterodimeric receptor results in a compound with mGlu2/2 homodimer selectivity. (2020) (4)
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: development of a [3.3.0]-based series and other piperidine bioisosteres. (2014) (4)
Activation of M1 muscarinic receptors reduce pathology and slow progression of neurodegenerative disease (2021) (3)
Regulation of Ion Channels and Neurotransmitter Release by Protein Kinase C (1990) (3)
Physiological Roles of Multiple Metabotropic Glutamate Receptor Subtypes in the Rat Basal Ganglia (2001) (3)
Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5. (2019) (3)
Difference in mGluR5 Interaction between Positive Allosteric Modulators from Two Structural Classes (2003) (3)
The Roles of Metabotropic Glutamate Receptors in Modulating the Activity of the Subthalamic Nucleus (2002) (3)
Permissive antagonism induced by novel allosteric antagonists of metabotropic glutamate receptor 7 (2006) (3)
Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy. (2016) (3)
Erratum to “Potent mGluR5 antagonists: Pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series” [Bioorg. Med. Chem. Lett. 21 (2011) 3243–3247] (2012) (3)
The First 50 Years of Molecular Pharmacology (2015) (3)
Pure Positive Allosteric Modulators (PAMs) of mGlu5 with Competitive MPEP-Site Interaction (2013) (3)
Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype. (2017) (2)
Allosteric Modulators of Metabotropic Glutamate Receptor 5 for Treatment of Schizophrenia (2011) (2)
Discovery of VU6028418: A Highly Selective and Orally Bioavailable M4 Muscarinic Acetylcholine Receptor Antagonist. (2021) (2)
Metabotropic Glutamate Receptors in the Globus Pallidus (2002) (2)
Positive allosteric modulation of metabotropic glutamate receptor 5 modulates Akt and GSK3β signaling in vivo (2019) (2)
Activation of Group II Metabotropic Glutamate Receptors (mGluR2 and mGluR3) as a Novel Approach for Treatment of Schizophrenia (2010) (2)
Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5. (2018) (2)
The Role of Aldehyde Oxidase and Xanthine Oxidase in the Biotransformation of a Novel Negative Allosteric Modulator of mGlu5 (2012) (2)
Development of the First CNS penetrant M5 Positive Allosteric Modulator (PAM) Based on a Novel, non-Isatin Core (2015) (2)
Extended Probe Characterization: Development of an M4 PAM with Improved Activity and Brain Exposure, while Avoiding Species Bias (2013) (2)
Identification of a Selective Allosteric Agonist of mGlu5 (2013) (2)
Synthesis and SAR of a series of mGlu7 NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core. (2020) (2)
Metabotropic glutamate receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database (2019) (2)
SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M4 PAMs. (2019) (2)
Huixian Wu Bound to an Allosteric Modulator Structure of a Class C GPCR Metabotropic Glutamate Receptor (2014) (2)
Development and characterization of a highly selective M5 PAM probe molecule with improved potency (2013) (2)
Evaluation of Synthetic Cytochrome P450-Mimetic Metalloporphyrins To Facilitate “Biomimetic” Biotransformation of a Series of mGlu5 Allosteric Ligands (2019) (2)
Unique serotonin receptor (5HT-1C) in choroid plexus is linked to phosphoinositide hydrolysis (1986) (2)
Discovery of “Molecular Switches” within a Series of mGlu5 Allosteric Ligands Driven by a “Magic Methyl” Effect Affording Both PAMs and NAMs with In Vivo Activity, Derived from an M1 PAM Chemotype (2021) (2)
Allosteric Modulators of Metabotropic Glutamate Receptors as Novel Therapeutics for Neuropsychiatric Disease (2022) (2)
Discovery of a novel metabotropic glutamate receptor 4 (mGlu4) positive allosteric modulator (PAM) extended probe (2013) (2)
Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder. (2022) (2)
Development and kilogram-scale synthesis of mGlu5 negative allosteric modulator VU0424238 (auglurant) (2017) (1)
Glutamate Receptors, Metabotropic (2013) (1)
Novel allosteric modulators of metabotropic glutamate receptors subtypes 2 and 5 for the treatment of schizophrenia (2008) (1)
mGlur5 positive allosteric modulators facilitate both LTP and LTD induction in the rat hippocampal CA1 region (2008) (1)
Discovery of the first selective M4 muscarinic acetylcholine receptor antagonists with in vivo anti-parkinsonian and anti-dystonic efficacy (2020) (1)
Influence of M1 muscarinic acetylcholine receptor activation on arousal and cognitive performance using electroencephalography and novel touchscreen cognition assessment (845.5) (2014) (1)
Microwave synthesis of [18F]FPEB in a semi-automated synthesis module (2010) (1)
Towards the treatment of Alzheimer's disease: Discovery and development of novel subtype-specific M1 allosteric agonists (2009) (1)
An allosteric potentiator suggests a role for M4 muscarinic acetylcholine receptor (mAChR) in modulating excitatory hippocampal synaptic transmission (2008) (1)
Effects of the M4 muscarinic receptor positive allosteric modulator VU0467154 on cognition and pyramidal cell firing properties in layer V of the mPFC (845.9) (2014) (1)
Discovery of a novel structural class of M4 positive allosteric modulators: Characterization of ML293, N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicotinamide, with CNS exposure in rats (2013) (1)
Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation s (2015) (1)
Identification of a high affinity MPEP-site silent allosteric modulator (SAM) for the metabotropic glutamate subtype 5 receptor (mGlu5) (2015) (1)
Physiological roles of multiple mGluR subtypes in rat hippocampus (1996) (1)
Molecular Pharmacology in the Postgenomic Era (2006) (1)
Discovery and optimization of a novel CNS penetrant series of mGlu4 PAMs based on a 1,4-thiazepane core with in vivo efficacy in a preclinical Parkinsonian model. (2021) (1)
Schild analyses reveal that the cerebral cortical serotonin 5HT/sub 2/ site is linked to phosphoinositide (PI) hydrolysis: relative efficacies of piperazines (1986) (1)
Pharmacological Treatments for Autism Spectrum Disorder: Will Emerging Approaches Yield New Treatments? (2016) (1)
Development of a Second Generation mGlu3 NAM Probe (2013) (1)
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) anatgonists (2008) (0)
Figure 4, Ca2+ mobilization screen with M5-CHO cells using 10 μM test compound in the presence of a submaximal concentration of Ach (~EC20) to triage libraries 3 and 5 for PAM activity (2013) (0)
MAOS Protocols for the General Synthesis and Lead Optimization of 3,6‐Disubstituted‐[1,2,4]triazolo[4,3‐b]pyridazines. (2009) (0)
allosteric modulator Modulation of neuronal microcircuit activities within the medial prefrontal cortex by mGluR 5 positive (2014) (0)
Figure 5, CRC overlay for CID 2145491 (2013) (0)
Efficacy of negative allosteric modulators of mGlu2 and mGlu3 in a rodent model of Major depressive disorder (2018) (0)
Figure 3, Calcium mobilization assays in rat M4/Gqi5-expressing CHO cells (2013) (0)
Table 4, In vivo Cassette clearance and in vitro pharmacokinetic values of selected compounds (2013) (0)
Microsoft Word-32670823-file00.docx (2013) (0)
Figure 2, Prior Art: M5 PAM probe molecules ML129 and ML172 (2013) (0)
Metabotropic glutamate receptors in GtoPdb v.2021.3 (2021) (0)
Figure 3, Stability of ML182 (2013) (0)
Characterization of novel selective positive allosteric modulators (PAMS) of the M4 muscarinic acetylcholine receptor (mAChR) (2008) (0)
Corrigendum to "Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: Development of a [3.3.0]-based series and other piperidine bioisosteres" [Bioorg. Med. Chem. Lett. 24 (2014) 1062-1066]. (2017) (0)
A Cyclic AMP-Dependent Form of Associative Synaptic Induced by Coactivation of ,&Adrenergic Receptors and Metabotropic Glutamate Receptors in Rat Hippocampus Plasticity (1994) (0)
Ventral Tegmental Area M5 Muscarinic Receptors Mediate Effort-Choice Responding and Nucleus Accumbens Dopamine in a Sex-Specific Manner (2023) (0)
Table 6, Calculated property comparison between the M5 probes and MDDR compounds (2013) (0)
Identification of novel allosteric modulators of mGlu5 acting at site distinct from MPEP binding. (2019) (0)
Figure 1, (−)-PHCCC, the prototypical mGluR4 PAM – weak, non-selective, poor physiochemical properties and no CNS penetration (2013) (0)
Figure 3, Modifications to the isatin core of ML129 (2013) (0)
Preview : Published ahead of advance online publication (2015) (0)
OPTIMIZATION OF NOVEL M1 PAMS FOR CLINICAL DEVELOPMENT WITH ENHANCED EFFICACY WHILE AVOIDING ADVERSE EFFECT LIABILITY FOR THE TREATMENT OF ALZHEIMER’S DISEASE (2019) (0)
Synthesis and Characterization of Chiral 6-Azaspiro[2.5]Octanes as Potent and Selective Antagonists of the M4 Muscarinic Acetylcholine Receptor (2021) (0)
Table 3, Fold shift data for selected compounds (2013) (0)
202. Roles of metabotropic glutamate receptors in the hippocampus (1996) (0)
Figure 2, Human (A) and rat (B) mGlu4 PAM CRC’s for ML292 (2013) (0)
Studies on the binding of [ 3 H]NMS in human cortex from subjects with schizophrenia and age sex matched controls: Different outcomes with the allosteric modulator BQCA. (2020) (0)
MAOS ls for the general synthesis and lead optimization of 3,6-disubstituted-[1,2,4]triazolo[4,3-b]pyridazines. (2009) (0)
Table 3, 5-CF3O isatin analogs (2013) (0)
Figure 4, Previously reported non-MPEP site mGluR5 PAMs and ML332 (2013) (0)
in the Hippocampus Receptors Persistently Active Metabotropic Glutamate Reduction of Excitatory Postsynaptic Responses by (2015) (0)
Discovery of a potent, selective and orally active in vivo mGlu4 positive allosteric modulator (2013) (0)
Table 2, Ricerca Profiling of ML337 (2013) (0)
Figure 5, Structures of mGlu3 NAMs RO4491533 (1) and LY2399575 (2), both dual mGlu2/mGlu3 NAMs (2013) (0)
Figure 1, Synthesis of Probe ML253 (2013) (0)
2 Running Title Page (2004) (0)
Discovery of a highly M5-preferring muscarinic acetylcholine receptor allosteric potentiator (2009) (0)
Figure 2, Structures of mGlu3 NAMs RO4491533 (1) and LY2399575 (2), both dual mGlu2/mGlu3 NAMs, and the first mGlu3 selective NAM, ML289, with ~15-fold selectivity versus mGlu2 (2013) (0)
Table 3, SAR Analysis for M1 Positive Allosteric Modulators (2013) (0)
Allosteric modulators of metapotropic glutamate receptor subtype 5 as a novel approach for treatment of CNS disorders (2008) (0)
THE USE OF COGNITIVE AND ERP BIOMARKERS OF CHOLINERGIC FUNCTION IN NOVEL TESTS OF MUSCARINIC POSITIVE ALLOSTERIC MODULATORS (2019) (0)
Discovery and Characterization of a Novel Subtype‐Selective M1 Allosteric Agonist for the Treatment of Alzheimer's Disease (2009) (0)
Figure 6, CRC overlay of muscarinic rM1 – rM5 selectivity profile for ML326 (VU0467903) (2013) (0)
SELECTIVE POTENTIATION OF MUSCARINIC ACETYLCHOLINE RECEPTOR SUBTYPE 1 DEMONSTRATES EFFICACY AND SAFETY IN PRECLINICAL MODELS OF ALZHEIMER'S DISEASE (2016) (0)
Acute administration of a novel M1 receptor allosteric potentiator (BQCA) restores reversal learning in a transgenic mouse model of Alzheimer's disease (Tg2576) (2009) (0)
Figure 2, LY2033298 and cheminformatics and database mining approach which lead to the first M4 probe compound (CID 864492) (2013) (0)
[Table, Synthetic procedure (large scale) and spectral data for ML172 (CID 44602489)]. (2013) (0)
Effects of the M 4 positive allosteric modulator VU 0467154 on cognition and electrophysiological properties in the mPFC in a rodent model of NMDA receptor hypofunction (2015) (0)
P2.105 The development of positive allosteric modulators of mGluR4 for the treatment of Parkinson's disease (2009) (0)
The discovery and characterization of a centrally penetrant (ML396) and a peripherally restricted (ML397) pan-Group III mGlu positive allosteric modulators (2015) (0)
Table 1, Stability of ML337 (2013) (0)
Figure 4, Comparison of the key profiles of the known M4 PAM art and ML253 (2013) (0)
Contribution of both M1 and M4 receptors to muscarinic agonist-mediated attenuation of the cocaine discriminative stimulus in mice (2011) (0)
Correction to “Dissociation of Protein Kinase-Mediated Regulation of Metabotropic Glutamate Receptor 7 (mGluR7) Interactions with Calmodulin and Regulation of mGluR7 Function” (2013) (0)
Figure 1, 2-(N-(2-chloro-5-(trifluoromethyl)phenyl)methylsulfonamido)-N-(cyclopropylmethyl)acetamide (ML332) (2013) (0)
Figure 1, CRCs at M1–M5 for HTS lead CID 3008304 (2013) (0)
Running title : Context-dependent pharmacology of mGluR 7 antagonists (2009) (0)
Microsoft Word-39700264-file00 (2009) (0)
Scheme 1, Synthesis of Analogues 8a and 9 (2013) (0)
Figure 6, Calcium mobilization assays in human M4/Gq15-expressing CHO cells (2013) (0)
Effects of M1 and M4 muscarinic acetylcholine receptor positive allosteric modulators on sleep and cognition in rodents (2013) (0)
Human class C G protein-coupled metabotropic glutamate receptor 1 in complex with a negative allosteric modulator (2014) (0)
Table 2, Human and Rat mGlu4 potency and % GluMax response (as normalized to standard PHCCC) for selected western amide analogs (2013) (0)
Figure 6, Concentration-response curves in Ca2+ mobilization assays with M1-,M2Gqi5-, M3, M4/Gqi5-, and M5-CHO cells for CID 44602489 (M5 EC50 = 1.9 μM) (2013) (0)
Localization and Physiological Roles of Metabotropic Glutamate Receptors in the Indirect Pathway (2002) (0)
Corrigendum to "Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides" [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179-5184]. (2018) (0)
Jeffrey Conn-Opportunities and Challenges for Drug Discovery in a Postgenomic World (2007) (0)
Figure 3, Human and rat M4 PAM CRCs of ML253 as assessed using calcium mobilization assays (2013) (0)
The Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator ADX88178 Inhibits Inflammatory Responses in Primary Microglia (2016) (0)
P4-680 A SELECTIVE INHIBITOR OF THE IMMUNOPROTEASOME ATTENUATES DISEASE PROGRESSION IN MOUSE MODELS OFALZHEIMER’S DISEASE (2019) (0)
Figure 2, Two MLPCN probe molecules derived from CID 3008304 (2013) (0)
Figure 1, M4 HTS hits (2010) (0)
Figure 2, Stability of ML253 (2013) (0)
Table 1, Stability of ML182 (2013) (0)
Development of the First Highly Selective mAChR 5 (M5) Positive Allosteric Modulator (PAM) (2013) (0)
43. BUILDING ON GENETICS AND PATHOPHYSIOLOGY OF SCHIZOPHRENIA TO GUIDE DISCOVERY OF NEW TREATMENTS (2018) (0)
Scheme 2, Probe preparation of ML337 (2013) (0)
Figure 7, ACh fold shift determinations for ML326 (VU0467903) and ML129 (VU0238429), at 30 μM, on the rM5 receptor (2013) (0)
Table 2, Methyl isatin analogs (2013) (0)
Novel Positive Allosteric Modulators Bias Acetylcholine Signaling at Human M4 Muscarinic Receptors (2013) (0)
Figure 4, Oxidative O-dealkylation of ML289 in rat and human liver microsomes (2013) (0)
M4 muscarinic acetylcholine receptor modulation of associative learning and behavioral flexibility in a novel touchscreen cognitive assessment (845.8) (2014) (0)
Table 1, Active heterocyclic biaryl analogs (2013) (0)
DMD052662 2066..2075 (2013) (0)
Receptors | Glutamate Receptors, Metabotropic (2021) (0)
Table 1, Assays and AIDs (2013) (0)
Figure 5, In vivo efficacy of ML182 (SID 99309089) in haloperidol induced catalepsy after PO dosing (2013) (0)
Corrigendum to “Development of a scintillation proximity assay for analysis of Na+/Cl− -dependent neurotransmitter transporter activity” [Anal. Biochem. 321 (2003) 31–37] (2012) (0)
Discovery, Synthesis, SAR 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 anti-Parkinsonian Animal Model (2011) (0)
Figure 1, Effects and profile of 5MPEP in vitro (2015) (0)
Figure 7, Calcium mobilization assays in a) M1, b) M2/Gqi5, c) M3, and M5 expressing CHO cells (2013) (0)
Table 5, Pan Labs profiling of ML326 and selected results for ML172 (2013) (0)
Figure 4, HTS single-point hit (2013) (0)
Muscarinic acetylcholine receptors in the etiology and treatment of schizophrenia (2020) (0)
Microsoft Word-JSD_3A4_activation_mGlu5_PAM_revised_final_V4[1] (2013) (0)
Scheme 2, Reagents and conditions: (a) K2CO3, KI, CAN, mw, 160 °C, 10 min (68%) (2013) (0)
Development of the First Potent, Selective and CNS penetrant M5 Negative Allosteric Modulator (NAM) (2014) (0)
Development of a Novel, Orthosteric M5 Antagonist Possessing a High Degree of Muscarinic Subtype Selectivity (2015) (0)
Figure 2, Complete Synthesis of ML289 (2013) (0)
Selective potentiation of muscarinic acetylcholine receptor subtype 1 demonstrates efficacy and safety in preclinical models of Alzheimer's disease and schizophrenia (2018) (0)
Graphical contents list (2013) (0)
Muscarinic modulation of hippocampal function in m1 knockout mice (1999) (0)
Figure 3, In vitro molecular pharmacology characterization of ML289 (2013) (0)
Table 1, Ricerca Profiling of ML289 (2013) (0)
Table 2, Summary of mGlu4 PAM probe molecules (2013) (0)
Figure 5, Reversal of amphetamine-induced hyper locomotion rat behavioral study (2013) (0)
Figure 3, Optimization strategy for CID 42633508, a highly M5-preferring PAM (2013) (0)
[Table, Synthetic procedure (large scale) and spectral data for ML173 (CID 45142486)]. (2013) (0)
CHAPTER 10:Glutamate Approaches Towards the Treatment of Mood Disorders (2012) (0)
Hyperactive Striatal Dopamine Signaling Observed in Huntington’s Disease Mouse Models Prior to Motor Symptom Onset Can be Attenuated via Activation of M4 Receptors (2022) (0)
Table 1, Structure and SAR for Analogues 12a (2013) (0)
Epileptiform Discharges in Hippocampal Slices Role of Synaptic Metabotropic Glutamate Receptors in (2015) (0)
43.1 GENETIC INSIGHTS LEAD TO DISCOVERY OF SELECTIVE ACTIVATORS OF MGLU1 AND MGLU3 METABOTROPIC GLUTAMATE RECEPTORS AS POTENTIAL TREATMENTS FOR SCHIZOPHRENIA (2018) (0)
Figure 1, Synthetic procedure and spectral data for ML254 (CID 46926631, SID 125305189) (2013) (0)
Table 4, SAR Analysis for rat M4 Positive Allosteric Modulators (2013) (0)
Analogs of 2- (4-heterociclilbencil) isoindolin-1-one compounds as positive allosteric modulators of muscarinic acetylcholine receptor M1 (2012) (0)

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