5-HT1 选择性抑制剂 | 激动剂 | 拮抗剂 | 调节剂;5-HT1 Selective Inhibitors | Agonists | Antagonists | Modulators;;InformationLasmiditan succinate (COL-144, LY573144) is a novel, centrally acting, highly selective5-HT(1F) receptoragonist (Ki=2.21 nM) without vasoconstrictor activity.Targets5-HT(1F) (Cell-free assay) 2.21 nM(Ki)In vitroLasmiditan shows higher selectivity for the 5-HT(1F) receptor relative to other 5-HT(1) receptor subtypes than the first generation 5-HT(1F) receptor agonist LY334370.In vivoLasmiditan is orally active in two in vivo models of migraine that involve electrical stimulation of the trigeminal ganglion. After oral administration, lasmiditan potently decreases dural plasma protein extravasation and the number of c-fos positive cells in the trigeminal nucleus caudalis at a dose of 3 mg/kg.