期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 10, 页码 3377-3384出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm9003818
关键词
-
The discovery of a series of pyrrole-sulfonamides as positive allosteric modulators (PAM) of alpha 7 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 0 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 0 nAChRs.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据