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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: 1 to 10 of 51

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Differential Pharmacology and Binding of mGlu Receptor Allosteric Modulators.
O'Brien DE, Shaw DM, Cho HP, Cross AJ, Wesolowski SS, Felts AS, Bergare J, Elmore CS, Lindsley CW, Niswender CM, Conn PJ
(2018) Mol Pharmacol 93: 526-540
MeSH Terms: Allosteric Regulation, Allosteric Site, Animals, Cell Line, Glutamic Acid, HEK293 Cells, Humans, Ligands, Mutagenesis, Protein Binding, Radioligand Assay, Rats, Receptors, Metabotropic Glutamate
Added March 3, 2020
0 Communities
1 Members
0 Resources
MeSH Terms
In vivo evaluation of IGF1R/IR PET ligand [F]BMS-754807 in rodents.
Prabhakaran J, Dewey SL, McClure R, Simpson NR, Tantawy MN, Mann JJ, Pham W, Kumar JSD
(2017) Bioorg Med Chem Lett 27: 941-943
MeSH Terms: Animals, Fluorine Radioisotopes, Heterografts, Humans, Mice, Positron-Emission Tomography, Pyrazoles, Radioligand Assay, Rats, Receptor, IGF Type 1, Receptor, Insulin, Triazines
Added March 21, 2018
0 Communities
2 Members
0 Resources
12 MeSH Terms
Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators.
Gregory KJ, Velagaleti R, Thal DM, Brady RM, Christopoulos A, Conn PJ, Lapinsky DJ
(2016) ACS Chem Biol 11: 1870-9
MeSH Terms: Acetylene, Allosteric Regulation, Click Chemistry, HEK293 Cells, Humans, Ligands, Photoaffinity Labels, Radioligand Assay, Receptor, Metabotropic Glutamate 5
Added April 6, 2017
0 Communities
1 Members
0 Resources
9 MeSH Terms
VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy.
Nickols HH, Yuh JP, Gregory KJ, Morrison RD, Bates BS, Stauffer SR, Emmitte KA, Bubser M, Peng W, Nedelcovych MT, Thompson A, Lv X, Xiang Z, Daniels JS, Niswender CM, Lindsley CW, Jones CK, Conn PJ
(2016) J Pharmacol Exp Ther 356: 123-36
MeSH Terms: Allosteric Regulation, Animals, Anti-Anxiety Agents, Astrocytes, Behavior, Animal, Brain, Dose-Response Relationship, Drug, Drug Discovery, GABA Agonists, HEK293 Cells, Humans, Inositol Phosphates, MAP Kinase Signaling System, Membrane Potentials, Mice, Mice, Inbred C57BL, Picolinic Acids, Pyridines, Radioligand Assay, Rats, Receptor, Metabotropic Glutamate 5, Synaptic Transmission
Added February 18, 2016
0 Communities
3 Members
0 Resources
22 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
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).
Turlington M, Noetzel MJ, Chun A, Zhou Y, Gogliotti RD, Nguyen ED, Gregory KJ, Vinson PN, Rook JM, Gogi KK, Xiang Z, Bridges TM, Daniels JS, Jones C, Niswender CM, Meiler J, Conn PJ, Lindsley CW, Stauffer SR
(2013) J Med Chem 56: 7976-96
MeSH Terms: Acetylene, Allosteric Regulation, Amides, Animals, Binding, Competitive, Cell Membrane, Drug Discovery, Excitatory Postsynaptic Potentials, HEK293 Cells, Hippocampus, Humans, Male, Models, Chemical, Models, Molecular, Molecular Structure, Picolinic Acids, Protein Structure, Tertiary, Radioligand Assay, Rats, Rats, Sprague-Dawley, Receptor, Metabotropic Glutamate 5, Structure-Activity Relationship
Added January 24, 2015
1 Communities
4 Members
0 Resources
22 MeSH Terms
Extracellular loop II modulates GTP sensitivity of the prostaglandin EP3 receptor.
Natarajan C, Hata AN, Hamm HE, Zent R, Breyer RM
(2013) Mol Pharmacol 83: 206-16
MeSH Terms: Animals, Dinoprostone, Guanosine 5'-O-(3-Thiotriphosphate), HEK293 Cells, Humans, Point Mutation, Protein Conformation, Rabbits, Radioligand Assay, Receptors, Prostaglandin E, EP3 Subtype, Signal Transduction
Added December 21, 2013
1 Communities
3 Members
0 Resources
11 MeSH Terms
Total synthesis and biological evaluation of phidianidines A and B uncovers unique pharmacological profiles at CNS targets.
Brogan JT, Stoops SL, Lindsley CW
(2012) ACS Chem Neurosci 3: 658-64
MeSH Terms: Animals, CHO Cells, Cell Proliferation, Cell Survival, Central Nervous System Agents, Chromatography, High Pressure Liquid, Cricetinae, Cricetulus, Dopamine Plasma Membrane Transport Proteins, Gastropoda, Guanosine 5'-O-(3-Thiotriphosphate), HEK293 Cells, Humans, Indicators and Reagents, Indole Alkaloids, Ligands, Oxadiazoles, Radioligand Assay, Receptors, Opioid, mu, Serotonin Plasma Membrane Transport Proteins, Structure-Activity Relationship
Added March 7, 2014
1 Communities
1 Members
0 Resources
21 MeSH Terms
Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.
Gregory KJ, Noetzel MJ, Rook JM, Vinson PN, Stauffer SR, Rodriguez AL, Emmitte KA, Zhou Y, Chun AC, Felts AS, Chauder BA, Lindsley CW, Niswender CM, Conn PJ
(2012) Mol Pharmacol 82: 860-75
MeSH Terms: Allosteric Regulation, Allosteric Site, Animals, Calcium, Glutamic Acid, HEK293 Cells, Humans, Mitogen-Activated Protein Kinase 1, Mitogen-Activated Protein Kinase 3, Phosphorylation, Point Mutation, Radioligand Assay, Rats, Receptor, Metabotropic Glutamate 5, Receptors, Metabotropic Glutamate, Structure-Activity Relationship
Added September 12, 2013
1 Communities
5 Members
0 Resources
16 MeSH Terms
Synthesis and pharmacological characterization of a novel sigma receptor ligand with improved metabolic stability and antagonistic effects against methamphetamine.
Seminerio MJ, Robson MJ, Abdelazeem AH, Mesangeau C, Jamalapuram S, Avery BA, McCurdy CR, Matsumoto RR
(2012) AAPS J 14: 43-51
MeSH Terms: Administration, Oral, Animals, Behavior, Animal, Benzothiazoles, Binding Sites, Central Nervous System Stimulants, Dose-Response Relationship, Drug, Half-Life, Injections, Intraperitoneal, Ligands, Male, Methamphetamine, Mice, Motor Activity, Piperazines, Protein Binding, Radioligand Assay, Receptors, sigma, Sulfur Compounds
Added July 10, 2013
0 Communities
1 Members
0 Resources
19 MeSH Terms