Lasmiditan hydrochloride CAS 613677-28-4

Name

Lasmiditan hydrochloride

Synonyms

COL 144 hydrochloride;LY 573144 hydrochloride;COL-144 hydrochloride;LY-573144 hydrochloride;COL144 hydrochloride;LY573144 hydrochloride

Molecular Structure

Molecular Structure of Lasmiditan hydrochloride CAS 613677-28-4

Molecular Formula

C19H19ClF3N3O2

Molecular Weight

413.82

CAS Number (Or Watson Number for Non-CAS Products)

613677-28-4

EINECS

Specs/Standards

99%min

Use

Lasmiditan (COL-144; LY573144) 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) Target: 5-HT1F receptor in 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 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. 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 ¦ÌM [1]. 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) [1]. Two RCTs in the phase II development of lasmiditan was reviewed. In the intravenous placebo-controlled RCT, lasmiditan doses of 2.5-45 mg were used, and there was a linear association between headache relief (HR) rates and dose levels (P < 0.02). For lasmiditan 20 mg, HR was 64 % and for placebo it was 45 % (NS). In the oral placebo-controlled RCT, lasmiditan doses of 50, 100, 200 and 400 mg were used. For HR, all doses of lasmiditan were superior to placebo (P < 0.05). For lasmiditan 400 mg, HR was 64 % and it was 25 % for placebo. Adverse events (AEs) emerging from the treatment were reported by 22 % of the patients receiving placebo and by 65, 73, 87 and 87 % of patients receiving 50, 100, 200 and 400 mg, respectively.

Links

This product is developed by our R&D company Caming Pharmaceutical Ltd (http://www.caming.com/), and here is the corresponding link http://caming.com/Lasmiditan-hydrochloride-cas-613677-28-4/

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This product is for research and development purpose only which may not be used directly as drugs, food, cosmetics or for any other non-R&D purpose. It may be toxic or hazardous, and should be handled only by qualified individuals trained in laboratory procedures. The buyer will be responsible to warn and inform any person that may be in contact with the product of the potential risks and hazards, as well as to ensure that purchase, use and disposal of the product comply with local laws and regulations.