"目录号: HY-14861A
GPCR/G ProteinNeuronal Signaling-
Lasmiditan hydrochloride 是一个高选择性的5-HT1F受体激动剂（Ki=2.1 nM），在5-HT(1B) 和5-HT(1D) 受体上Ki值分别是1043 nM和1357 nM.
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生物活性
Description
Lasmiditan hydrochloride is a high-affinity, highly selective 5-HT1F receptor agonist (Ki=2.1 nM), compared with Ki of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively.IC50 value: 2.1 nM (Ki, 5-HT1F); >1000 nM (Ki, 5-HT1B/5-HT1D) [1]Target: 5-HT1F receptorin vitro: In vitro binding studies Lasmiditan showed a K(i) value of 2.21 nM at the 5-HT(1F) receptor, compared with K(i) values of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively, a selectivity ratio greater than 470-fold. Lasmiditan show 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. Unlike the 5-HT(1B/1D) receptor agonist sumatriptan, lasmiditan did not contract rabbit saphenous vein rings, a surrogate assay for human coronary artery constriction, at concentrations up to 100 μM.in vivo: 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).
Clinical Trial
CoLucid Pharmaceuticals-FGK Clinical Research GmbH
Migraine Disorders
July 2009
Phase 2
CoLucid Pharmaceuticals
Migraine
October 2006
Phase 2
CoLucid Pharmaceuticals
Pharmacokinetics
April 20, 2017
Phase 1
Eli Lilly and Company
Healthy
June 16, 2017
Phase 1
CoLucid Pharmaceuticals
Migraine
March 31, 2017
Phase 1
CoLucid Pharmaceuticals
Acute Treatment of Migraine in Adults
October 2015
Phase 3
CoLucid Pharmaceuticals
Bioavailability Under Fed and Fasted Conditions
January 2015
Phase 1
CoLucid Pharmaceuticals-SNBL Clinical Pharmacology Center, Inc.
Acute Treatment of Migraine
March 21, 2017
Phase 1
CoLucid Pharmaceuticals
Acute Migraine
April 2015
Phase 3
CoLucid Pharmaceuticals-Algorithme Pharma Inc
Migraine
March 14, 2017
Phase 1
CoLucid Pharmaceuticals
Acute Migraine
May 2016
Phase 3
CoLucid Pharmaceuticals-Algorithme Pharma Inc-Cognitive Research Corporation
Migraine
February 7, 2017
Phase 1
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