Ziprasidone HCl monohydrate
产品说明书
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同义名 : | 盐酸齐拉西酮水合物;齐拉西酮盐酸盐一水合物 ;CP-88,059; Ziprasidone (hydrochloride hydrate); CP 88059 hydrochloride monohydrate; Ziprasidone hydrochloride monohydrate |
| CAS号 : | 138982-67-9 | |
| 货号 : | A473367 | |
| 分子式 : | C21H24Cl2N4O2S | |
| 纯度 : | 97% | |
| 分子量 : | 467.41 | |
| MDL号 : | MFCD00921885 | |
| 存储条件： |
Pure form Inert atmosphere, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 25 mg/mL(53.49 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Ziprasidone HCl H2O is a full antagonist of D2 receptors and of 5-HT2A receptors and is a partial agonist of 5-HT1A receptors, of 5-HT2C receptors and 5-HT1D receptors, used as an atypical antipsychoticfor the treatment of schizophrenia as well as acute mania and mixed states associated with bipolar disorder. Ziprasidone HCl has high affinity for rat (Ki: 3.4 nM)/human (2.5 nM) 5-HT1A receptors, 5-HT2A (0.42 nM), and dopamine D2 receptors (4.8 nM). Ziprasidone HCl is an inhibitor of norepinephrine reuptake[2]. In vivo, ziprasidone antagonizes 5-HT2A receptor-induced head twitch with 6-fold higher potency than for blockade of d-amphetamine-induced hyperactivity, a measure of central dopamine D2 receptor antagonism. The compound is well tolerated in animals at doses producing effective dopamine antagonism in the brain[3]. Ziprasidone exhibits dose proportional, linear changes in exposure and is hepatically metabolized primarily by aldehyde oxidase[4]. Short-term treatment with intramuscular ziprasidone was effective and well tolerated in patients with acute agitation associated with psychosis[5]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01185743 | Schizophrenia ... 展开 >> Diabetes 收起 << | Phase 4 | Completed | - | Austria ... 展开 >> Medical University of Vienna Vienna, Austria, 1090 收起 << |
| NCT00538629 | - | Completed | - | - | |
| NCT01598324 | - | Terminated(Clinical trial from... 展开 >> which subjects were recruited closed to enrollment) 收起 << | - | United States, Massachusetts ... 展开 >> McLean Hospital - McLean Imaging Center Belmont, Massachusetts, United States, 02478 收起 << | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.14mL 0.43mL 0.21mL |
10.70mL 2.14mL 1.07mL |
21.39mL 4.28mL 2.14mL |
| 参考文献 |
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