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Ziprasidone hydrochloride monohydrate
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 hydrochloride monohydrate图片
CAS NO:138982-67-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
100mg电议

产品介绍
Ziprasidone (CP-88059) hydrochloride monohydrate 是一种具有口服活性的联合 5-HT 和多巴胺受体拮抗剂。
Cas No.138982-67-9
别名盐酸齐拉西酮水合物; CP 88059 hydrochloride monohydrate
化学名5-[2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethyl]-6-chloro-1,3-dihydroindol-2-one;hydrate;hydrochloride
Canonical SMILESC1CN(CCN1CCC2=C(C=C3C(=C2)CC(=O)N3)Cl)C4=NSC5=CC=CC=C54.O.Cl
分子式C21H24Cl2N4O2S
分子量467.41
溶解度≥ 11.7 mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.Target: 5-HT receptor; Dopamine receptorZiprasidone hydrochloride monohydrate is the salt form of ziprasidone, which possesses an in vitro 5-HT2A/dopamine D2 receptor affinity ratio higher than any clinically available antipsychotic agent. In vivo, Ziprasidone hydrochloride monohydrate 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 hydrochloride monohydrate also has high affinity for the 5-HT1A, 5-HT1D and 5-HT2C receptor subtypes, which may further enhance its therapeutic potential [1]. Ziprasidone hydrochloride monohydrate 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 hydrochloride monohydrate, and are thus unlikely to contribute to its antipsychotic effects [2]. Ziprasidone hydrochloride monohydrate 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].Clinical indications: Bipolar I disorder; Bipolar disorder; Mania; SchizophreniaFDA Approved Date: February 2001

References:
[1]. Papakostas GI, Petersen TJ, Nierenberg AA, et al. Ziprasidone augmentation of selective serotonin reuptake inhibitors (SSRIs) for SSRI-resistant major depressive disorder. The Journal of Clinical Psychiatry. 2004, 65(2):217-221.
[2]. Paul E. Keck, Marcio Versiani, Steven Potkin, et al. Ziprasidone in the Treatment of Acute Bipolar Mania: A Three-Week, Placebo-Controlled, Double-Blind, Randomized Trial. Am J Psychiatry 2003;160:741-748.
[3]. Glen L. Stimmel, Mary A. Gutierrez, Vivian Lee. Ziprasidone: An atypical antipsychotic drug for the treatment of schizophrenia. Clinical Therapeutics, 2002, 24(1):21-37.
[4]. Anne W Schmidt, Lorraine A Lebel, Harry R Howard Jr. et al. Ziprasidone: a novel antipsychotic agent with a unique human receptor binding profile. European Journal of Pharmacology. 2001,425(3):197-201.
[5]. Ziprasidone