P. jeffrey Conn
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P. jeffrey Conn's AcademicInfluence.com Rankings
P. jeffrey Connmedical Degrees
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#1299
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#1625
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Pharmacology
#95
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#123
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P. jeffrey Conn's Degrees
- PhD Pharmacology Vanderbilt University
- Bachelors Pharmacy University of Kentucky
Why Is P. jeffrey Conn Influential?
(Suggest an Edit or Addition)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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