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 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 RD com­pa­ny Cam­ing Phar­ma­ceu­ti­cal Ltd (http://​www​.cam​ing​.com/), and here is the cor­re­spond­ing link http://​cam​ing​.com/​L​a​s​m​i​d​i​t​a​n​-​h​y​d​r​o​c​h​l​o​r​i​d​e​-​c​a​s​-​6​1​3​6​7​7​-​2​8​-4/

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