Lasmiditan(COL-144,LY573144)是一種首創(chuàng)的(first-in-class),新型的,高度選擇性的5-HT(1F)受體激動(dòng)劑,體外結(jié)合研究表明5-HT(1F)受體的Ki值為2.21 nM??捎糜谄^痛的相關(guān)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).
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