| Literature DB >> 19419141 |
Ramin Faghih1, Sujatha M Gopalakrishnan, Jens Halvard Gronlien, John Malysz, Clark A Briggs, Caroline Wetterstrand, Hilde Ween, Michael P Curtis, Kathy A Sarris, Gregory A Gfesser, Rachid El-Kouhen, Holly M Robb, Richard J Radek, Kennan C Marsh, William H Bunnelle, Murali Gopalakrishnan.
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.Entities:
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Year: 2009 PMID： 19419141 DOI： 10.1021/jm9003818
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446