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).

Gentry PR, Kokubo M, Bridges TM, Noetzel MJ, Cho HP, Lamsal A, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR
J Med Chem. 2014 57 (18): 7804-10

PMID: 25147929 · PMCID: PMC4175000 · DOI:10.1021/jm500995y

MeSH Terms (14)

Allosteric Regulation Animals Central Nervous System Drug Discovery Drug Evaluation, Preclinical High-Throughput Screening Assays Humans Indazoles Male Piperidines Rats Receptor, Muscarinic M5 Substrate Specificity Sulfonamides

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