Pimethixene maleate (Synonyms: 匹美噻吨马来酸盐; Pimetixene maleate)
目录号: PL14987 纯度: ≥99%
CAS No. :13187-06-9
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中文名称
Pimethixene maleate
中文别名
1-甲基-4-[噻吨酮-9-基]马来酸哌啶;Pimethixene马来;马来酸甲哌硫蒽;匹美噻吨 马来酸盐;1-甲基-4-(噻吨-9-亚基)哌啶;匹美噻吨马来酸盐
英文名称
Pimethixene maleate
英文别名
9-(1-Methyl-4-piperidylene)thioxanthene maleate;1-METHYL-4-[THIOXANTHEN-9-YLIDENE]PIPERIDINE MALEATE SALT;PIMETHIXEN MALEATE SALT;1-methyl-4-(9H-thioxanthen-9-ylidene)piperidinium hydrogen maleate;1-Methyl-4-(thioxanthen-9-ylidene)piperidine;9-(1-methyl-4-piperidylene)-thioxanthenmaleate;9-(n-methyl-piperidyliden-4)thioxanemaleate;bp-400;PIMETHIXENE MALEATE;Pimethixene maleic salt;PIMETHIXENE MALEATE SALT;9-(1-methyl-4-piperidylene)thioxanthenemaleate;Pimetixene maleate;Pimethixene maleate
Cas No.
13187-06-9
分子式
C19H19NS.C4H4O4
分子量
409.50
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
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。
生物活性
Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene maleate is a highly potent antagonist of 5-HT 1A , 5-HT 2A , 5-HT 2B , 5-HT 2C , histamine H 1 , dopamine D 2 and D 4.4 as well as muscarinic M 1 and M 2 receptors, with pK i s of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.
性状
Solid
IC50 & Target[1][2]
5-HT1A Receptor 7.63 (pKi) 5-HT2A Receptor
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (244.20 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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