Click here to close Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly. We suggest using a current version of Chrome, FireFox, or Safari.
XB-ART-40086
J Med Chem 2009 May 28;5210:3377-84. doi: 10.1021/jm9003818.
Show Gene links Show Anatomy links

Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.

Faghih R , Gopalakrishnan SM , Gronlien JH , Malysz J , Briggs CA , Wetterstrand C , Ween H , Curtis MP , Sarris KA , Gfesser GA , El-Kouhen R , Robb HM , Radek RJ , Marsh KC , Bunnelle WH , Gopalakrishnan M .


???displayArticle.abstract???
The discovery of a series of pyrrole-sulfonamides as positive allosteric modulators (PAM) of alpha7 nAChRs is described. Optimization of this series led to the identification of 19 (A-867744), a novel type II PAM with good potency and selectivity. Compound 19 showed acceptable pharmacokinetic profile across species and brain levels sufficient to modulate alpha7 nAChRs. In a rodent model of sensory gating, 19 normalized gating deficits. These results suggest that 19 represents a novel class of molecules capable of allosteric modulation of the alpha7 nAChRs.

???displayArticle.pubmedLink??? 19419141
???displayArticle.link??? J Med Chem


Species referenced: Xenopus laevis
Genes referenced: pam