Ziprasidone hydrochloride monohydrate

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(In Vitro):Ziprasidone hydrochloride monohydrate (0-500 nM, 150 seconds) blocks wild-type hERG current.(In Vivo):Ziprasidone hydrochloride monohydrate (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.

Ziprasidone hydrochloride monohydrate (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 hydrochloride monohydrate (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

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

138982-67-9

467.4119

C21H24Cl2N4O2S

>98% (HPLC)

10 mM in DMSO

O=C1CC2=CC(CCN3CCN(C4=NSC5=C4C=CC=C5)CC3)=C(Cl)C=C2N1.Cl.O

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

(-20℃)

With Ice Pack

≥ 2 years