Edvinsson L
Department of Internal Medicine, Lund University Hospital, Lund, Sweden.
CNS Drugs. 2001;15(10):745-53. doi: 10.2165/00023210-200115100-00001.
Cerebral blood vessels are innervated by sensory nerves that store several neurotransmitters. In primary headaches, there is a clear association between head pain and the release of the neuropeptide calcitonin gene-related peptide (CGRP). Furthermore, when triptan antimigraine agents are administered, headache subsides and the neuropeptide release normalises, in part via a presynaptic effect. The central role of CGRP in primary headaches has led to the search for suitable antagonists of the receptors for this neuropeptide, which it is hoped will have less cardiovascular adverse effects than the triptans. Recently, the initial pharmacological profile of such a group of compounds has been disclosed. These compounds are small molecules with high selectivity for human CGRP receptors. Hypothetically, these agents will be efficacious in the relief of migraine headaches via blockade of the effects of CGRP.
脑血管由储存多种神经递质的感觉神经支配。在原发性头痛中，头痛与神经肽降钙素基因相关肽（CGRP）的释放之间存在明确关联。此外，给予曲坦类抗偏头痛药物时，头痛缓解且神经肽释放恢复正常，部分是通过突触前效应实现的。CGRP在原发性头痛中的核心作用促使人们寻找该神经肽受体的合适拮抗剂，希望其心血管不良反应比曲坦类药物少。最近，这类化合物的初步药理学特征已被披露。这些化合物是对人CGRP受体具有高选择性的小分子。据推测，这些药物将通过阻断CGRP的作用有效缓解偏头痛。
