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抑制剂描述:

产品名称:Chlorprothixene hydrochloride

产品别名:见爱必信官网

英文别名:Chlorprothixene hydrochloride

靶点:5-HT Receptor;Dopamine;H1 receptor;mAChR

CAS:6469-93-8

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Chlorprothixene is a typical antipsychotic drug of the thioxanthene (tricyclic) class. Chlorprothixene exerts strong blocking effects by blocking the 5-HT2 D1, D2, D3, histamine H1, muscarinic and alpha1 adrenergic receptors.

溶解性:Ethanol : 25 mg/mL (70.96 mM; Need ultrasonic)
DMSO : 2.5 br>mg/mL (7.10 mM; Need ultrasonic)

体外研究:

Chlorprothixene exihibited strong binding affinities to dopamine and histamine receptors, The Ki values of D1, D2, D3, D5 and H1 were 18nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM, respectively. Chlorprothixene showed little affinity to H3 with the Ki value of >1000 nM. In COS-7 cells transiently expressed rat 5-HT7 receptors and HEK-293 cells stably transfected with rat 5-HT6, the Ki values of chlorprothixene were 5.6 nM and 3 nM, respectively. In Vero 76 cells, chlorprothixene treatment inhibited SARS-CoV replication, 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.

体内研究: In rat brain depressing the release of hypothalamic and hypophyseal hormones, chlorprothixene blocked postsynaptic mesolimbic dopaminergic D1 and D2 receptors. Chlorprothixene treatment restored normal ceramide concentrations in murine bronchial epithelial cells, reduced inflammation in the lungs of mice with cystic fibrosis (CF) and prevented infection with Pseudomonas aeruginosa.

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