降钙素基因相关肽
狨猴
敌手
三叉神经节
药理学
偏头痛
受体
体内
刺激
化学
医学
神经科学
内分泌学
内科学
神经肽
生物
古生物学
生物技术
感觉系统
作者
Henri Doods,Gerhard Hallermayer,Dongmei Wu,Michael Entzeroth,K Rudolf,Wolfhard Engel,Wolfgang Eberlein
标识
DOI:10.1038/sj.bjp.0703110
摘要
Calcitonin gene‐related peptide (CGRP) is one of the most potent 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 14.4±6.3 ( n =4) pM. In an in vivo model, BIBN4096BS in doses between 1 and 30 μg 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. British Journal of Pharmacology (2000) 129 , 420–423; doi: 10.1038/sj.bjp.0703110
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