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。
| 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 |
|---|
| Formula | C21H21ClN4OS·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 Code | O=C1NC2=C(C=C(CCN3CCN(C4=NSC5=CC=CC=C45)CC3)C(Cl)=C2)C1.[H]Cl |
|---|
| Synonyms | CP-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 Vivo | Ziprasidone 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 model | Rats |
|---|
| Formulation & Dosage | N/A |
|---|
| References | Biochem Pharmacol. 2006 Jan 12;71(3):278-86; Eur J Pharmacol. 2004 Nov 28;505(1-3):253-4. |
|---|
m.cnreagent.com