Pimethixene maleate 是抗组胺和抗血清素剂，用作抗偏头疼剂。Pimethixene maleate 为高效的多靶点拮抗剂，对 5-HT1A，5-HT2A，5-HT2B，5-HT2C，组胺 H1，多巴胺 D2 和 D4.4 以及毒蕈碱 M1 和 M2 的 pKi 值分别为 7.63，10.22，10.44，8.42，10.14，8.19，7.54，8.61 和 9.38。
货号:ajcx39302
CAS:13187-06-9
分子式:C23H23NO4S
分子量：409.5
溶解度:DMSO : 100 mg/mL (244.20 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively[1].

[1]. Schmitz B, et al. BF-1--a novel selective 5-HT2B receptor antagonist blocking neurogenic dural plasma protein extravasation in guinea pigs. Eur J Pharmacol. 2015 Mar 15;751:73-80.

Protocol:

5-HT1AReceptor 7.63(pKi)

5-HT2AReceptor 10.22(pKi)

5-HT2BReceptor 10.44(pKi)

5-HT2CReceptor 8.42(pKi)

D2receptor 8.19(pKi)

DD4.4receptor 7.54(pKi)

M1receptor 8.61(pKi)

M2receptor 9.38(pKi)