Ontology highlight
ABSTRACT:
SUBMITTER: Hogenkamp DJ
PROVIDER: S-EPMC3912855 | biostudies-literature | 2013 Nov
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20131030 21
A series of novel arylpyrid-3-ylmethanones (7a-aa) were designed as modulators of α7 nicotinic acetylcholine receptors (nAChRs). The methanones were found to be type I positive allosteric modulators (PAMs) of human α7 nAChRs expressed in Xenopus ooctyes. Structure-activity relationship (SAR) studies resulted in the identification of compound 7v as a potent and efficacious type I PAM with maximum modulation of a nicotine EC5 response of 1200% and EC50 = 0.18 μM. Compound 7z was active in reversin ...[more]