Ziprasidone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

D2 和 5-HT2A 受体的完全拮抗剂，Ki 分别为 6.8 和 0.6 nM；也是 5-HT1A 受体的部分激动剂，以及 5-HT2C 和 5-HT1D 受体的部分拮抗剂。

A full antagonist of D2 and 5-HT2A receptors with Ki of 6.8 and 0.6 nM, respectively; also is a partial agonist of 5-HT1A, and a partial antagonist of 5-HT2C and 5-HT1D receptors; exhibits potent antipsychotic activity in vivo.Schizophrenia Approved.

Ziprasidone (0-500 nM, 150 seconds) blocks wild-type hERG current.Cell Viability Assay 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).

Ziprasidone (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. Animal Model:Eight-week-old female Sprague-Dawleyrats weighing 200 to 250 g 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).

CP 88059 | CP-88059 | CP88059

GPCR/G Protein

5-HT Receptor

5-HTtransporter|5-HT1A|5-HT1B|5-HT1D|5-HT2A|5-HT2C|5-HT6|5-HT7|D1|D2|D3|H1receptor|norepinephrinetransporter(NET)|α1A-adrenergicreceptor|α2A-adrenergicreceptor

Neurological Disease

Schizophrenia

146939-27-7

412.9356

C21H21ClN4OS

>98% (HPLC)

10 mM in DMSO

ClC1=C(CCN2CCN(CC2)C2=NSC3=CC=CC=C23)C=C2CC(=O)NC2=C1

2H-Indol-2-one, 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-

(-20℃)

With Ice Pack

≥ 2 years