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(Ki=4.8 nM)、5-HT2A(Ki=0.42 nM) 和5-HT1A(Ki=3.4 nM) 有亲和作用。

Ziprasidone (CP-88059) mesylate is an orally active combined 5-HT and dopamine receptor antagonist [1]. Ziprasidone mesylate has affinities for Rat D 2 ( K i =4.8 nM), 5-HT 2A ( K i =0.42 nM) and 5-HT 1A ( K i =3.4 nM) [1].

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 (IC 50 = 120 nm).

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).

185021-64-1

C22H25ClN4O4S2

509.04

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years