Hay Debbie L, Poyner David
School of Biological Sciences, University of Auckland, Auckland, New Zealand.
Cardiovasc Drug Rev. 2005 Spring;23(1):31-42. doi: 10.1111/j.1527-3466.2005.tb00155.x.
CGRP is an important neuropeptide found throughout the cardiovascular system. However, until recently it has been difficult to define its pharmacology or physiological role because of the lack of suitable antagonists. BIBN4096BS is a high-affinity, nonpeptide antagonist that shows much greater selectivity for human CGRP1 receptors compared to any other drug. Its pharmacology has been defined with studies on transfected cells or cell lines endogenously expressing receptors of known composition. These have allowed confirmation that in many human blood vessels, CGRP is working via CGRP1 receptors. However, it also interacts with other CGRP-activated receptors, of unknown composition. In vivo, clinical studies have shown that BIBN4096BS is likely to be useful in the treatment of migraine. It has also been used to define the role of CGRP in phenomena such as plasma extravasation and cardioprotection following ischemia.
降钙素基因相关肽（CGRP）是一种在整个心血管系统中发现的重要神经肽。然而，直到最近，由于缺乏合适的拮抗剂，很难确定其药理学或生理作用。BIBN4096BS是一种高亲和力的非肽拮抗剂，与任何其他药物相比，它对人CGRP1受体表现出更高的选择性。其药理学已通过对转染细胞或内源性表达已知组成受体的细胞系的研究得以确定。这些研究证实，在许多人体血管中，CGRP是通过CGRP1受体发挥作用的。然而，它也与其他成分未知的CGRP激活受体相互作用。在体内，临床研究表明BIBN4096BS可能对偏头痛治疗有用。它还被用于确定CGRP在诸如缺血后血浆外渗和心脏保护等现象中的作用。
