Edvinsson L
Department of Internal Medicine, Lund University Hospital, Lund, Sweden.
Cephalalgia. 2004 Aug;24(8):611-22. doi: 10.1111/j.1468-2982.2003.00719.x.
In primary headaches, there is a clear association between the headache and the release of calcitonin gene-related peptide (CGRP) but not with any of the other neuronal messengers. The purpose of this review is to describe the role of CGRP in the intracranial circulation and to elucidate a possible role for a specific CGRP receptor antagonist in the treatment of primary headaches. Acute treatment with a 5-HT(1B/1D) agonist (triptan) results in alleviation of the headache and normalization of the cranial venous CGRP levels, in part due to a presynaptic inhibitory effect on sensory nerves. The central role of CGRP in migraine and cluster headache pathophysiology has led to the search for small molecule CGRP antagonists with few cardiovascular side-effects. The initial pharmacological profile of such a group of compounds has recently been disclosed. One of these compounds has been found to be efficacious in the relief of acute attacks of migraine.
在原发性头痛中,头痛与降钙素基因相关肽(CGRP)的释放之间存在明确关联,但与其他任何神经递质均无关联。本综述的目的是描述CGRP在颅内循环中的作用,并阐明特定CGRP受体拮抗剂在原发性头痛治疗中的可能作用。用5-羟色胺(1B/1D)激动剂(曲坦类药物)进行急性治疗可缓解头痛并使颅内静脉CGRP水平恢复正常,部分原因是对感觉神经的突触前抑制作用。CGRP在偏头痛和丛集性头痛病理生理学中的核心作用促使人们寻找心血管副作用少的小分子CGRP拮抗剂。最近已披露了这类化合物的初步药理学特征。已发现其中一种化合物对缓解偏头痛急性发作有效。