您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > Ziprasidone HCl(CP-88059)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Ziprasidone HCl(CP-88059)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ziprasidone HCl(CP-88059)图片
CAS NO:122883-93-6
规格:≥98%
包装与价格:
包装价格(元)
250mg电议
500mg电议
1g电议
2g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)449.4
FormulaC21H21ClN4OS·HCl
CAS No.122883-93-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 90 mg/mL (200.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES CodeO=C1NC2=C(C=C(CCN3CCN(C4=NSC5=CC=CC=C45)CC3)C(Cl)=C2)C1.[H]Cl
SynonymsCP-88059; CP88059; CP88059 mesylate; Ziprasidone mesylate, CP 88059; CP-88,059; CP-88,059-01; Geodon; Zeldox; Zipwell.
实验参考方法
In Vitro

In vitro activity: Ziprasidone has high affinity for human 5-HT receptors and for human dopamine D(2) receptors. Ziprasidone is a 5-HT(1A) receptor agonist and an antagonist at 5-HT(2A), 5-HT(2C) and 5-HT(1B/1D) receptors. Ziprasidone inhibits neuronal uptake of 5-HT and norepinephrine comparable to the antidepressant imipramine. Ziprasidone blocks wild-type hERG current in a voltage- and concentration-dependent manner with IC(50) of 120nM in stably transfected HEK-293 cells. Ziprasidone shows minimal tonic block of hERG current estimated during a depolarizing voltage (-20 or +30mV) or evaluated by the envelope of tails test (+30mV). Ziprasidone significantly increases the time constant of the slow component of hERG current deactivation (at -50mV).

In VivoZiprasidone exhibits less potent block of wild-type hERG current with IC(50) of 2.8 mM in Xenopus oocytes. Ziprasidone suppresses the significant increases in food intake produced by olanzapine, indicating that it has an intrinsic protective mechanism against drug-induced increases in food intake in rats. Ziprasidone results in a notable increase in NGF and ChAT immunoreactivity in the dentate gyrus (DG), CA1, and CA3 areas of the hippocampus of rats. Ziprasidone dose-dependently slows raphe unit activity (ED50 = 300 mg/kg i.v.) as does the atypical antipsychotics clozapine (ED50 = 250 mg/kg i.v.) and olanzapine (ED50 = 1000 mg/kg i.v.) in anesthetized rats.
Animal modelRats
Formulation & DosageN/A
References

Biochem Pharmacol. 2006 Jan 12;71(3):278-86; Eur J Pharmacol. 2004 Nov 28;505(1-3):253-4.