您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Chlorprothixene
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
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
规格:≥98%
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)315.86
FormulaC18H18ClNS
CAS No.113-59-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 6 mg/mL (19 mM)
Water: <1 mg/mL
Ethanol: 28 mg/mL (88.6 mM)
Other info

Chemical Name: 1-Propanamine, 3-(2-chloro-9H-thioxanthen-9-ylidene)-N,N-dimethyl-, (Z)-

InChi Key: WSPOMRSOLSGNFJ-AUWJEWJLSA-N

InChi Code: InChI=1S/C18H18ClNS/c1-20(2)11-5-7-14-15-6-3-4-8-17(15)21-18-10-9-13(19)12-16(14)18/h3-4,6-10,12H,5,11H2,1-2H3/b14-7-

SMILES Code: CN(C)CC/C=C1C2=C(SC3=C\1C=CC=C3)C=CC(Cl)=C2

Synonyms

MK 184; N 714; N 714C; NSC 1872;0 Paxyl; Rentovet; Ro 4-0403; N-714; MK-184; Taractan; Tarasan; Chlorprothixene

实验参考方法
In Vitro

In vitro activity: Chlorprothixene 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). 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. Administration of chlorprothixene results in inhibition of SARS-CoV replication in Vero 76 cells, with IC50 of 16.7 μM for Urbani strain, 13.0 μM for Frankfurt-1, 18.5 μM for CHUK-W1 and 15.8 μM for Toronto-2. There are similar to those detected with promazine.

In VivoChlorprothixene blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain depressing the release of hypothalamic and hypophyseal hormones. High dose of chlorprothixene inhibits the protection afforded by iproniazid against the reserpine-induced release of catecholamines in adrenal medulla and brain as well as the decrease of 5HT, NE and DA due to reserpine or iproniazid in rat brain. 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).
Animal modelB6.129P2 (CF/3)-CftrTgH(neoim)Hgu (abbreviated CFMHH) congenic mice.
Formulation & DosageDissolved in 0.9% NaCl solution, final concentration 8 mg/L; 1 mL every time; Five 10-minute inhalations, every 12 hours
References

Bioorg Med Chem Lett. 2009 Jan 15;19(2):538-42; J Pharmacol Exp Ther. 1961 Jul;133:18-24.