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Chlorprothixene
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Chlorprothixene图片
CAS NO:113-59-7
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
50mg电议

产品介绍
Chlorprothixene 是一种多巴胺和组胺受体拮抗剂，对 hD1、hD2、hD3、hD5 和 hH1 受体的 Kis 分别为 18 nM、2.96 nM、4.56 nM、9 nM 和 3.75 nM。
Cas No.113-59-7
别名氯普噻吨
化学名(3Z)-3-(2-chlorothioxanthen-9-ylidene)-N,N-dimethylpropan-1-amine
Canonical SMILESCN(C)CCC=C1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl
分子式C18H18ClNS
分子量315.87
溶解度≥ 15.79mg/mL in Ethanol
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Chlorprothixene has strong binding affinities to dopamine and histamine receptors, such as D1, D2, D3, D5, H1, 5-HT2, 5-HT6 and 5-HT7, with Ki of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM and 5.6 nM, respectively.Target: Dopamine ReceptorChlorprothixene exerts strong binding affinities to the dopamine and histamine receptors, such as D1, D2, D3, D5 and H1 with Ki values of 18nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM, respectively, but has little affinity to H3 (Ki >1000 nM) [1]. Chlorprothixene also shows high affinities for both rat 5-HT6 from stably transfected HEK-293 cells, and rat 5-HT7 receptors from transiently expressed COS-7 cells, with Ki values of 3 nM and 5.6 nM, respectively [2].Administration of Chlorprothixene restores normal ceramide concentrations in murine bronchial epithelial cells, reduces inflammation in the lungs of mice with cystic fibrosis (CF) and prevents infection with Pseudomonas aeruginosa, by inhibiting acidsphingomyelinase (Asm) and not neutral sphingomyelinase (Nsm) [3].

References:
[1]. von Coburg, Y., et al., Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. Bioorg Med Chem Lett, 2009. 19(2): p. 538-42.
[2]. Roth, B.L., et al., Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther, 1994. 268(3): p. 1403-10.
[3]. Becker, K.A., et al., Acid sphingomyelinase inhibitors normalize pulmonary ceramide and inflammation in cystic fibrosis. Am J Respir Cell Mol Biol, 2010. 42(6): p. 716-24.