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5-HT(1)-like receptor agonists and the pathophysiology of migraine.
Trends in Pharmacological Sciences ( IF 13.9 ) Pub Date : 1989-05-01 , DOI: 10.1016/0165-6147(89)90238-1
P R Saxena 1 , M D Ferrari
Affiliation  

Recently, AG-25086 and GR-43175 have been reported to be highly effective in aborting acute migraine attacks. These compounds seem selectively to stimulate a sub-population of 5-HT(1)-like receptors to inhibit noradrenaline release from certain sympathetic neurovascular terminals, to contract dog saphenous vein and dog, monkey and human basilar arteries, and to decrease the arteriovenous anastomotic component of carotid blood flow in the cat. GR-43175 neither has any antinociceptive effect nor crosses the blood-brain barrier. Pramod Saxena and Michel Ferrari review the clinical effectiveness of these 5-HT(1)-like receptor agonists and their selective pharmacology, both of which strongly suggest that excessive dilatation in the extracerebral cranial (scalp and/or dural) vasculature is an integral part of the pathophysiology of migraine.

中文翻译:

5-HT(1)样受体激动剂和偏头痛的病理生理学。

最近,据报道AG-25086和GR-43175在中止急性偏头痛发作方面非常有效。这些化合物似乎选择性刺激5-HT(1)-样受体的亚群,抑制去甲肾上腺素从某些交感神经血管末端释放,收缩犬大隐静脉和犬,猴和人基底动脉,并减少动静脉吻合。猫颈动脉血流的组成部分。GR-43175既没有抗伤害作用,也没有穿过血脑屏障。普拉莫德·萨克森纳(Pramod Saxena)和米歇尔·法拉利(Michel Ferrari)综述了这些5-HT(1)-样受体激动剂的临床疗效及其选择性药理作用,两者均强烈暗示大脑外颅(头皮和/或硬脑膜)血管过度扩张是不可或缺的一部分偏头痛的病理生理学。
更新日期:2019-11-01
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