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.

Felts AS, Rodriguez AL, Morrison RD, Bollinger KA, Venable DF, Blobaum AL, Byers FW, Thompson Gray A, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA
Bioorg Med Chem Lett. 2017 27 (21): 4858-4866

PMID: 28958625 · PMCID: PMC5716465 · DOI:10.1016/j.bmcl.2017.09.042

MeSH Terms (18)

Allosteric Regulation Amides Animals Cell Membrane Permeability Dogs Dopamine Plasma Membrane Transport Proteins Drug Evaluation, Preclinical Half-Life Humans Inhibitory Concentration 50 Madin Darby Canine Kidney Cells Mice Microsomes, Liver Pyridines Rats Receptor, Metabotropic Glutamate 5 Structure-Activity Relationship Triazoles

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