Goadsby P J
Institute of Neurology, Queen Square, London,
Clin Neurosci. 1998;5(1):18-23.
The development of serotonin (5HT) agonists that have highly specific receptor profiles has fueled the study of 5HT receptor pharmacology and in particular the pharmacology of the 5HT1 sub-class of receptors. The currently accepted classification of 5HT receptors includes seven classes known as 5HT1 through 5HT7 and the class most implicated in migraine 5HT1, which consists of the A, B, D, E, and F sub-types. Currently, effective and relatively specific anti-migraine compounds, as a group, are potent 5HT1B/1D agonists. Their possible mechanisms of action include carotid territory vasoconstrictor effects and inhibitory effects on both the peripheral and central terminals of the trigeminal innervation of the pain-producing intracranial structures. Future drug development will target these individual mechanisms to dissect out which, if any, determines the clinical efficacy of the compounds.
具有高度特异性受体谱的5-羟色胺(5HT)激动剂的开发推动了5HT受体药理学的研究,尤其是5HT1受体亚类的药理学研究。目前公认的5HT受体分类包括7类,称为5HT1至5HT7,以及与偏头痛关系最为密切的5HT1类,它由A、B、D、E和F亚型组成。目前,作为一个整体,有效且相对特异的抗偏头痛化合物是强效5HT1B/1D激动剂。它们可能的作用机制包括颈动脉区域血管收缩作用以及对产生疼痛的颅内结构三叉神经支配的外周和中枢终末的抑制作用。未来的药物开发将针对这些个体机制,以弄清楚哪些(如果有的话)决定了这些化合物的临床疗效。