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The publication data currently available has been vetted by Vanderbilt faculty, staff, administrators and trainees. The data itself is retrieved directly from NCBI's PubMed and is automatically updated on a weekly basis to ensure accuracy and completeness.

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Results: 21 to 30 of 98

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Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).
Martín-Martín ML, Bartolomé-Nebreda JM, Conde-Ceide S, Alonso de Diego SA, López S, Martínez-Viturro CM, Tong HM, Lavreysen H, Macdonald GJ, Steckler T, Mackie C, Bridges TM, Daniels JS, Niswender CM, Noetzel MJ, Jones CK, Conn PJ, Lindsley CW, Stauffer SR
(2015) Bioorg Med Chem Lett 25: 1310-7
MeSH Terms: Allosteric Regulation, Animals, Antipsychotic Agents, Brain, Drug Evaluation, Preclinical, Half-Life, Heterocyclic Compounds, 2-Ring, Humans, Imidazoles, Locomotion, Microsomes, Liver, Protein Binding, Pyrimidinones, Rats, Receptor, Metabotropic Glutamate 5, Structure-Activity Relationship
Added February 19, 2015
0 Communities
3 Members
0 Resources
16 MeSH Terms
Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles.
Rook JM, Tantawy MN, Ansari MS, Felts AS, Stauffer SR, Emmitte KA, Kessler RM, Niswender CM, Daniels JS, Jones CK, Lindsley CW, Conn PJ
(2015) Neuropsychopharmacology 40: 755-65
MeSH Terms: Allosteric Regulation, Amphetamine, Animals, Benzamides, Calcium, Cerebellum, Corpus Striatum, Dose-Response Relationship, Drug, HEK293 Cells, Humans, Locomotion, Male, Maze Learning, Niacinamide, Piperidines, Positron-Emission Tomography, Radioligand Assay, Rats, Receptor, Metabotropic Glutamate 5, Structure-Activity Relationship, Thiazoles
Added February 19, 2015
0 Communities
5 Members
0 Resources
21 MeSH Terms
Novel mGluR5 positive allosteric modulator improves functional recovery, attenuates neurodegeneration, and alters microglial polarization after experimental traumatic brain injury.
Loane DJ, Stoica BA, Tchantchou F, Kumar A, Barrett JP, Akintola T, Xue F, Conn PJ, Faden AI
(2014) Neurotherapeutics 11: 857-69
MeSH Terms: Allosteric Regulation, Animals, Brain Injuries, Cell Count, Cerebral Cortex, Disease Models, Animal, Glycine, Hippocampus, Male, Membrane Glycoproteins, Mice, Mice, Inbred C57BL, Microglia, Motor Activity, NADPH Oxidase 2, NADPH Oxidases, Neuroprotective Agents, Nitric Oxide Synthase Type II, Phenylacetates, Pyridines, Receptor, Metabotropic Glutamate 5, Recovery of Function, Thiazoles
Added February 19, 2015
0 Communities
1 Members
0 Resources
23 MeSH Terms
Modulation of neuronal microcircuit activities within the medial prefrontal cortex by mGluR5 positive allosteric modulator.
Pollard M, Bartolome JM, Conn PJ, Steckler T, Shaban H
(2014) J Psychopharmacol 28: 935-46
MeSH Terms: Action Potentials, Allosteric Regulation, Animals, Benzamides, Carbachol, Drug Synergism, Excitatory Amino Acid Agonists, Excitatory Amino Acid Antagonists, Inhibitory Postsynaptic Potentials, Male, Methoxyhydroxyphenylglycol, Neural Pathways, Prefrontal Cortex, Pyrazoles, Pyridines, Rats, Receptor, Metabotropic Glutamate 5, Receptors, Metabotropic Glutamate, Thiazoles
Added February 19, 2015
0 Communities
1 Members
0 Resources
19 MeSH Terms
Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
Bates BS, Rodriguez AL, Felts AS, Morrison RD, Venable DF, Blobaum AL, Byers FW, Lawson KP, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA
(2014) Bioorg Med Chem Lett 24: 3307-14
MeSH Terms: Allosteric Site, Animals, Anxiety, Disease Models, Animal, Dose-Response Relationship, Drug, Drug Discovery, Humans, Male, Mice, Molecular Structure, Picolinic Acids, Pyrazines, Rats, Rats, Sprague-Dawley, Receptor, Metabotropic Glutamate 5, Structure-Activity Relationship
Added February 19, 2015
0 Communities
3 Members
0 Resources
16 MeSH Terms
Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency.
Turlington M, Noetzel MJ, Bridges TM, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Tong HM, Macdonald GJ, Daniels JS, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR
(2014) Bioorg Med Chem Lett 24: 3641-6
MeSH Terms: Allosteric Regulation, Animals, Cell Line, Dose-Response Relationship, Drug, Drug Discovery, Humans, Ligands, Molecular Structure, Piperidones, Pyrazoles, Rats, Receptor, Metabotropic Glutamate 5, Structure-Activity Relationship
Added February 19, 2015
0 Communities
3 Members
0 Resources
13 MeSH Terms
Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅).
Turlington M, Malosh C, Jacobs J, Manka JT, Noetzel MJ, Vinson PN, Jadhav S, Herman EJ, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Martín-Martín ML, Tong HM, López S, MacDonald GJ, Steckler T, Daniels JS, Weaver CD, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR
(2014) J Med Chem 57: 5620-37
MeSH Terms: Allosteric Regulation, Animals, Antipsychotic Agents, HEK293 Cells, Humans, Microsomes, Liver, Naphthyridines, Rats, Receptor, Metabotropic Glutamate 5, Schizophrenia, Structure-Activity Relationship
Added February 16, 2015
0 Communities
4 Members
0 Resources
11 MeSH Terms
Head-to head comparison of mGlu1 and mGlu5 receptor activation in chronic treatment of absence epilepsy in WAG/Rij rats.
D'Amore V, Santolini I, Celli R, Lionetto L, De Fusco A, Simmaco M, van Rijn CM, Vieira E, Stauffer SR, Conn PJ, Bosco P, Nicoletti F, van Luijtelaar G, Ngomba RT
(2014) Neuropharmacology 85: 91-103
MeSH Terms: Animals, Anticonvulsants, Blotting, Western, Cerebral Cortex, Disease Models, Animal, Drug Tolerance, Electrodes, Implanted, Electroencephalography, Epilepsy, Absence, Excitatory Amino Acid Agents, Male, Mice, Transgenic, Niacinamide, Rats, Rats, Inbred ACI, Rats, Wistar, Receptor, Metabotropic Glutamate 5, Receptors, Metabotropic Glutamate, Thalamus, Time Factors
Added May 27, 2014
0 Communities
1 Members
0 Resources
20 MeSH Terms
Radiation Dosimetry of (18)F-FPEB in Humans.
Kessler RM, Seibyl J, Cowan RL, Zald D, Young JS, Ansari MS, Stabin MG
(2014) J Nucl Med 55: 1119-21
MeSH Terms: Adolescent, Adult, Female, Humans, Male, Middle Aged, Nitriles, Positron-Emission Tomography, Pyridines, Radiometry, Receptor, Metabotropic Glutamate 5, Whole Body Imaging, Young Adult
Added May 27, 2014
0 Communities
1 Members
0 Resources
13 MeSH Terms
Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site.
Gregory KJ, Nguyen ED, Malosh C, Mendenhall JL, Zic JZ, Bates BS, Noetzel MJ, Squire EF, Turner EM, Rook JM, Emmitte KA, Stauffer SR, Lindsley CW, Meiler J, Conn PJ
(2014) ACS Chem Neurosci 5: 282-95
MeSH Terms: Binding Sites, Computer Simulation, Molecular Docking Simulation, Mutagenesis, Site-Directed, Protein Binding, Protein Interaction Mapping, Receptor, Metabotropic Glutamate 5, Structure-Activity Relationship
Added January 24, 2015
1 Communities
3 Members
0 Resources
8 MeSH Terms