LasMiditan

Lasmiditan（COL-144，LY573144）是一种首创的（first-in-class），新型的，高度选择性的5-HT(1F)受体激动剂，体外结合研究表明5-HT(1F)受体的Ki值为2.21 nM。可用于偏头痛的相关研究。Lasmiditan (COL-144; LY573144) is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist, showed a K(i) value of 2.21 nM at the 5-HT(1F) receptor in vitro binding studies. Lasmiditan showed 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 two rodent models of migraine, oral administration of lasmiditan potently inhibited markers associated with electrical stimulation of the trigeminal ganglion (dural plasma protein extravasation, and induction of the immediate early gene c-Fos in the trigeminal nucleus caudalis).