选择性5-羟色胺1F受体激动剂lasmiditan

随着生活节奏的加快,偏头痛的发病率呈逐渐增加的趋势。目前用于治疗偏头痛的药物主要为曲坦类药物,但由于该类药物会使血管收缩,因此对于心脑血管和周围血管疾病患者禁用。曲坦类药物对中重度头痛患者的疗效显著降低。因此,迫切需要开发新的急性期治疗药物。lasmiditan是一种非曲坦类的5-HT1F受体激动剂,多项临床试验研究表明其具有良好的有效性和安全性。主要从lasmiditan的药物概况、相关背景、合成路线、药理作用、临床研究和安全性等方面进行介绍。

A selective 5-hydroxytryptamine1F receptor agonist: lasmiditan

With the accelerated pace of life, the incidence of migraine was gradually increasing. Currently, drugs mainly used in treatment of migraine are triptans. While triptans can constrict blood vessels, they are prohibited for patients with cardiovascular and peripheral vascular diseases. And triptans have lower efficacy for moderate and severe patients. Therefore, it is necessary to find a novel therapeutic drug. lasmiditan is a selective 5-HT_1F receptor agonist, and many clinical studies show that lasmiditan has a good effectiveness and safety. The drug situation, background, route of synthesis, pharmacological action, clinical trials researches, and safety of lasmiditan are reviewed in this paper.