针对偏头痛的靶向垂体腺苷酸环化酶激活肽疗法。
Targeted Pituitary Adenylate Cyclase-Activating Peptide Therapies for Migraine.
机构信息
Danish Headache Center and Department of Neurology, Rigshospitalet Glostrup, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2600, Glostrup, Copenhagen, Denmark.
出版信息
Neurotherapeutics. 2018 Apr;15(2):371-376. doi: 10.1007/s13311-017-0596-x.
Abstract
Here, we review the role of pituitary adenylate cyclase-activating peptide-38 (PACAP38) in migraine pathophysiology and data implicating PAC receptor as a future drug target in migraine. Much remains to be fully elucidated about migraine pathophysiology, but recent attention has focused on signaling molecule PACAP38, a vasodilator able to induce migraine attacks in patients who experience migraine without aura. PACAP38, with marked and sustained effect, dilates extracerebral arteries but not the middle cerebral artery. The selective affinity of PACAP38 to the PAC receptor makes this receptor a highly interesting and potential novel target for migraine treatment. Efficacy of antagonism of this receptor should be investigated in randomized clinical trials.
摘要
在这里，我们回顾了垂体腺苷酸环化酶激活肽-38（PACAP38）在偏头痛发病机制中的作用，以及 PAC 受体作为偏头痛未来药物靶点的数据。偏头痛发病机制仍有许多尚未完全阐明，但最近的研究重点是信号分子 PACAP38，它是一种血管扩张剂，能够在没有先兆的偏头痛患者中引发偏头痛发作。PACAP38 具有显著而持久的作用，可扩张颅外动脉，但不扩张大脑中动脉。PACAP38 对 PAC 受体的选择性亲和力使该受体成为偏头痛治疗的一个非常有趣和有潜力的新靶点。应该在随机临床试验中研究拮抗该受体的疗效。
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