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).

Gentry PR, Kokubo M, Bridges TM, Kett NR, Harp JM, Cho HP, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Wood MR, Lindsley CW
J Med Chem. 2013 56 (22): 9351-5

PMID: 24164599 · PMCID: PMC3876027 · DOI:10.1021/jm4013246

MeSH Terms (16)

Allosteric Regulation Animals Brain CHO Cells Cricetinae Cricetulus Drug Discovery Drug Evaluation, Preclinical Humans Imidazoles Indoles Male Rats Receptor, Muscarinic M5 Structure-Activity Relationship Substrate Specificity

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