期刊
BRITISH JOURNAL OF PHARMACOLOGY
卷 129, 期 3, 页码 420-423出版社
STOCKTON PRESS
DOI: 10.1038/sj.bjp.0703110
关键词
BIBN4096BS; CGRP-antagonist; migraine
Calcitonin gene-related peptide (CGRP) is one of the most patent endogenous vasodilators known. This peptide is increased during migraine attacks and has been implicated in the pathogenesis of migraine headache. Here we report on the first small molecule selective CGRP antagonist: BIBN4096BS. In vitro, this compound is extremely potent at primate CGRP receptors exhibiting an affinity (K-i) for human CGRP receptors of 14.1 +/- 6.3 (n = 4) phl. In an in vitro model, BIBN4096BS in doses between 1 and 30 mu g kg(-1) (i.v.) inhibited the effects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood flow in marmoset monkeys. It is concluded that BIBN4096BS is a potent and selective CGRP antagonist.
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