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首页> 外文期刊>Expert opinion on therapeutic targets >New therapeutic target in primary headaches - blocking theCGRP receptor.
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New therapeutic target in primary headaches - blocking theCGRP receptor.

机译：原发性头痛的新治疗靶点-阻断CGRP受体。

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摘要

The primary headaches are among the most prevalent neurological disorders, afflicting up to 16% of the adult population. The associated pain originates from intracranial blood vessels that are innervated by sensory nerves storing several neurotransmitters. In primary headaches, there is a clear association between the headache and the release of calcitonin gene-related peptide (CGRP), but not other neuronal messengers. The specific purpose of this review is to describe CGRP in the human cranial circulation and to elucidate a possible role for a specific antagonist in the treatment of primary headaches. Acute treatment with administration of a 5-HT(1B/1D) agonist (triptan) results in alleviation of the headache and normalisation of the CGRP level. The mechanism of action of triptans involves vasoconstriction of intracranial vessels and a presynaptic inhibitory effect of sensory nerves. The central role of CGRP in migraine and cluster headache pathophysiology has led to the search for small-molecule CGRPantagonists, which are predicted to have fewer cardiovascular side effects in comparison to the triptans. The initial pharmacological profile of such a group of compounds has recently been disclosed. These compounds have high selectivity for human CGRP receptors and are reportedly efficacious in the relief of acute attacks of migraine.
机译：原发性头痛是最普遍的神经系统疾病之一，困扰着多达16％的成年人口。相关的疼痛源自颅内血管，这些血管被储存了几种神经递质的感觉神经支配。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的关联，而其他神经元信使则没有。这篇综述的具体目的是描述人颅循环中的CGRP，并阐明特定拮抗剂在治疗原发性头痛中的可能作用。给予5-HT（1B / 1D）激动剂（曲普坦）的急性治疗可减轻头痛，并降低CGRP水平。曲普坦的作用机制涉及颅内血管的收缩和感觉神经的突触前抑制作用。 CGRP在偏头痛和丛集性头痛的病理生理中的核心作用导致人们寻求小分子CGRP拮抗剂，与曲普坦类药物相比，它们的心血管副作用较小。最近已经公开了这类化合物的初始药理学特征。这些化合物对人CGRP受体具有高选择性，据报道对缓解偏头痛的急性发作有效。

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