期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 12, 期 3, 页码 379-382出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(01)00761-2
关键词
-
Dihydropyridine 5a was found to be an inhibitor of neuropeptide Y-1 binding in a high throughput I-125-PYY screening assay. Structure-activity studies around certain portions of the dihydropyridine chemotype identified BMS-193885 (6e) as a potent and selective Y-1 receptor antagonist. In a forskolin-stimulated c-AMP production assay using CHO cells expressing the human Y-1 receptor, 6e demonstrated full functional antagonism (K-b = 4.5 nM). Compound 6e inhibited NPY-induced feeding in satiated rats when dosed at 3.0 and 10.0 mg/kg (ip), and also decreased spontaneous overnight food consumption in rats at doses of 10 and 20 mg/kg (ip). (C) 2002 Elsevier Science Ltd. All rights reserved.
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