Ziprasidone HCl
Ziprasidone(CP88059)盐酸盐是5-HT和多巴胺受体拮抗剂，有抗精神病活性。
中文名：盐酸齐拉西酮
英文名：Ziprasidone HCl; CP-88059 hydrochloride
CAS 号： 122883-93-6
分子式：C₂₁H₂₂Cl₂N₄OS
分子量：449.4
纯度：>98.0%
| Description | Ziprasidone Hcl(CP-88059 Hcl) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. Target: 5-HT receptor; Dopamine receptor Ziprasidone (hydrochloride) 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 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]. Clinical indications: Bipolar I disorder; Bipolar disorder; Mania; Schizophrenia FDA Approved Date: February 2001 |
| Target | 5-HT Receptor |
| 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. |
其他产品
相关产品
- Asenapine hydrochloride
- Tropisetron
- Cyproheptadine hydrochloride
- Quetiapine
- Idalopirdine
- SB-742457
- Olanzapine
- Naratriptan Hydrochloride
- Metergoline
- lurasidone
- Isocorynoxeine
- (Z)-Thiothixene
- Deramciclane
- Desipramine hydrochloride
- Dolasetron
- Eltoprazine
- Eptapirone
- Flibanserin
- Granisetron hydrochloride
- Iloperidone hydrochloride
- Iloperidone
