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Ziprasidone Sale

(Synonyms: 齐拉西酮; CP-88059) 目录号 : GC11020

齐拉西酮 (CP-88059) 是一种口服活性抗精神病药,是一种 5-HT 和多巴胺受体拮抗剂的组合。

Ziprasidone Chemical Structure

Cas No.:146939-27-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥368.00
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100mg
¥725.00
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产品描述

Ziprasidone (CP-88059) is a combined 5-HT (serotonin) and dopamine receptor antagonist. Ziprasidone exhibits potent effects of antipsychotic activity, and is used for treating various mental disorders including schizophrenia[1][2][3].

Ziprasidone possesses an in vitro 5-HT2A/dopamine D2 receptor affinity ratio higher than any clinically available antipsychotic agent. 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. Ziprasidone also has high affinity for the 5-HT1A, 5-HT1D and 5-HT2C receptor subtypes, which may further enhance its therapeutic potential[1]. Ziprasidone sulfoxide and sulfone were the major metabolites in human serum. The affinities of the sulfoxide and sulfone metabolites for 5-HT2 and D2 receptors are low with respect to ziprasidone, and are thus unlikely to contribute to its antipsychotic effects[2].Ziprasidone was associated with significant differential adverse effects relative to placebo in BPM, BPD, and schizophrenia with no significant difference in weight gain in all 3 groups. Self-reported somnolence was increased across the 3 conditions. Subjects with BPM were more vulnerable to EPS than those with BPD or schizophrenia[3].

References:
[1]. Seeger, T.F., et al., Ziprasidone (CP-88,059): a new antipsychotic with combined dopamine and serotonin receptor antagonist activity. J Pharmacol Exp Ther, 1995. 275(1): p. 101-13.
[2]. Prakash, C., et al., Metabolism and excretion of a new antipsychotic drug, ziprasidone, in humans. Drug Metab Dispos, 1997. 25(7): p. 863-72.
[3]. Gao, K., et al., Risk for adverse events and discontinuation due to adverse events of ziprasidone monotherapy relative to placebo in the acute treatment of bipolar depression, mania, and schizophrenia. J Clin Psychopharmacol, 2013. 33(3): p. 425-31.

Chemical Properties

Cas No. 146939-27-7 SDF
别名 齐拉西酮; CP-88059
化学名 5-[2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethyl]-6-chloro-1,3-dihydroindol-2-one
Canonical SMILES C1CN(CCN1CCC2=C(C=C3C(=C2)CC(=O)N3)Cl)C4=NSC5=CC=CC=C54
分子式 C21H21ClN4OS 分子量 412.94
溶解度 ≥ 20.647 mg/mL in DMSO with gentle warming 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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1 mg 5 mg 10 mg
1 mM 2.4217 mL 12.1083 mL 24.2166 mL
5 mM 0.4843 mL 2.4217 mL 4.8433 mL
10 mM 0.2422 mL 1.2108 mL 2.4217 mL
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