Ziprasidone mesylate

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CAS NO:

185021-64-1

CP-88059 mesylate

Ziprasidone (CP-88059) mesylate 是一种具有口服活性的5-HT和多巴胺 (dopamine) 受体拮抗剂。Ziprasidone mesylate 对大鼠D₂(K_i=4.8 nM)、5-HT_2A(K_i=0.42 nM) 和5-HT_1A(K_i=3.4 nM) 有亲和作用。

生物活性

Ziprasidone (CP-88059) mesylate is an orally active combined5-HTanddopaminereceptor antagonist^[1]. Ziprasidone mesylate has affinities for RatD₂(K_i=4.8 nM),5-HT_2A(K_i=0.42 nM) and5-HT_1A(K_i=3.4 nM)^[1].

IC₅₀& Target

Rat 5-HT₂Receptor

0.42 nM (Ki)

Rat 5-HT_1AReceptor

3.4 nM (Ki)

Rat D₂Receptor

4.8 nM (Ki)

体外研究
(In Vitro)

Ziprasidone mesylate (0-500 nM, 150 seconds) blocks wild-type hERG current^[2].

Cell Viability Assay^[2]

Cell Line:	HEK-293 cells
Concentration:	0-500 nM
Incubation Time:	150 seconds
Result:	Blocked wild-type hERG current in a voltage- and concentration-dependent manner (IC₅₀= 120 nm).

体内研究
(In Vivo)

Ziprasidone mesylate (oral gavage; 20 mg/kg; once daily; 7 weeks) results in weight loss, low level physical activity, high resting energy expenditure and greater capacity for thermogenesis when subjected to cold^[3].

Animal Model:	Eight-week-old female Sprague-Dawley rats weighing 200 to 250 g^[3]
Dosage:	20 mg/kg
Administration:	Oral gavage; 20 mg/kg; once daily; 7 weeks
Result:	Gained significantly less weight (P = 0.031), had a lower level of physical activity (P = 0.016), showed a higher resting energy expenditure (P< 0.001), and displayed a greater capacity for thermogenesis when subjected to cold (P< 0.001).

Clinical Trial

分子量

509.04

Formula

C₂₂H₂₅ClN₄O₄S₂

CAS 号

185021-64-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.