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Chlorprothixene

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Chemical Structure| 113-59-7 同义名 : -
CAS号 : 113-59-7
货号 : A371690
分子式 : C18H18ClNS
纯度 : 98%
分子量 : 315.86
MDL号 : MFCD00869180
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(110.81 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • D3 receptor

    D3 receptor, Ki:4.56 nM

  • D5 receptor

    D5 receptor, Ki:9 nM

  • D1 receptor

    D1 receptor, Ki:18 nM

  • D2 receptor

    D2 receptor, Ki:2.96 nM
描述 Chlorprothixene (CPTX) is an antipsychotic drug of the thioxanthene class. Chlorprothixene exerts strong binding affinities to the dopamine and histamine receptors, such as D1, D2, D3, D5 and H1 with Ki values of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM, respectively, but has little affinity to H3 (Ki >1000 nM)[1]. Chlorprothixene inhibited the proton currents in a concentration-dependent manner (IC50 = 1.7 μM). Chlorprothixene at 3 μM slightly shifted the activation voltage toward depolarization. Both the activation and the deactivation kinetics of the proton currents were slowed by chlorprothixene 1.2- and 3.5-fold, respectively. Thus, the inhibition of proton currents may be partly responsible for the antioxidant effects of thioxanthene antipsychotic drugs[3]. 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[4]. 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)[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.17mL

0.63mL

0.32mL

15.83mL

3.17mL

1.58mL

31.66mL

6.33mL

3.17mL
参考文献

[1]Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.Y. von Coburg, T. Kottke, L. Weizel, X. Ligneau, H. Stark Bioorg Med Chem Lett. 2009 Jan 15; 19(2): 538–542

[2]Roth BL, Craigo SC, et al. Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther. 1994 Mar;268(3):1403-10.

[3]Kim J, Song JH. Thioxanthenes, chlorprothixene and flupentixol inhibit proton currents in BV2 microglial cells. Eur J Pharmacol. 2016;779:31‐37

[4]Roth BL, Craigo SC, Choudhary MS, 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):1403‐1410

[5]Acid sphingomyelinase inhibitors normalize pulmonary ceramide and inflammation in cystic fibrosis. Katrin Anne Becker, Joachim Riethmüller, Anja Lüth, Gerd Döring, Burkhard Kleuser, Erich Gulbins Am J Respir Cell Mol Biol. 2010 Jun; 42(6): 716–724