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伊潘立酮

伊潘立酮用途

Iloperidone(HP 873)是D2/5-HT2受体拮抗剂,可作用于精神分裂症。

伊潘立酮名称

[ CAS 号 ]:
133454-47-4

[ 中文名 ]:
伊潘立酮

[ 英文名 ]:
Iloperidone

[英文别名 ]:

Zomaril
iloperidone
Fanapta
Fanapt

伊潘立酮生物活性

[ 描述 ]:

Iloperidone(HP 873)是D2/5-HT2受体拮抗剂,可作用于精神分裂症。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体

信号通路 >> 神经信号通路 >> 多巴胺受体

研究领域 >> 神经疾病

[参考文献]

[1]. Kongsamut, S., et al., Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol, 1996. 317(2-3): p. 417-23.

[2]. Sainati, S.M., et al., Safety, tolerability, and effect of food on the pharmacokinetics of iloperidone (HP 873), a potential atypical antipsychotic. J Clin Pharmacol, 1995. 35(7): p. 713-20.

[3]. Albers, L.J., A. Musenga, and M.A. Raggi, Iloperidone: a new benzisoxazole atypical antipsychotic drug. Is it novel enough to impact the crowded atypical antipsychotic market? Expert Opin Investig Drugs, 2008. 17(1): p. 61-75.

[相关活性小分子]

伊潘立酮物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
593.7±50.0 °C at 760 mmHg

[ 熔点 ]:
118-120°C

[ 分子式 ]:
C₂₄H₂₇FN₂O₄

[ 分子量 ]:
426.481

[ 闪点 ]:
312.8±30.1 °C

[ 精确质量 ]:
426.195496

[ PSA ]:
64.80000

[ LogP ]:
3.81

[ 外观性状 ]:
white to beige

[ 蒸汽压 ]:
0.0±1.7 mmHg at 25°C

[ 折射率 ]:
1.570

[ 储存条件 ]:
-20°C Freezer, Under Inert Atmosphere

[ 水溶解性 ]:
DMSO: soluble5mg/mL, clear

伊潘立酮MSDS

伊潘立酮安全信息

[ 符号 ]:

GHS02, GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H301 + H311 + H331-H370

[ 警示性声明 ]:
P210-P260-P280-P301 + P310-P311

[ 危害码 (欧洲) ]:
F,T

[ 风险声明 (欧洲) ]:
11-23/24/25-39/23/24/25

[ 安全声明 (欧洲) ]:
16-36/37-45

[ 危险品运输编码 ]:
UN2811 - class 6.1 - PG 3 - EHS - Toxic solids, organic, n.o.s., HI: all

[ RTECS号 ]:
KM5777850

[ 海关编码 ]:
2934999090

伊潘立酮合成路线

伊潘立酮上下游产品

伊潘立酮上游产品

伊潘立酮下游产品

伊潘立酮海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

伊潘立酮文献

A thorough QTc study of 3 doses of iloperidone including metabolic inhibition via CYP2D6 and/or CYP3A4 and a comparison to quetiapine and ziprasidone.

J. Clin. Psychopharmacol. 33(1) , 3-10, (2013)

The potential for iloperidone, a D2/5-HT2A antipsychotic, to affect the heart rate-corrected QT interval (QTc) was assessed in the absence and presence of metabolic inhibitors in a randomized, open-la...

Long-term safety and tolerability of iloperidone: results from a 25-week, open-label extension trial.

CNS Spectr. 18(1) , 43-54, (2013)

Long-term use of the atypical antipsychotic iloperidone has not been investigated at doses above 16 mg/d. This article describes safety and tolerability results from the 25-week open-label extension o...

Stable-isotope dilution LC-MS/MS assay for determination of iloperidone and its two major metabolites, P 88 and P 95, in human plasma: application to a bioequivalence study.

Bioanalysis 5(6) , 669-86, (2013)

Iloperidone is a novel antipsychotic drug with high affinity for serotonin and D(2) dopamine receptors. A sensitive and rapid isotope dilution LC-MS/MS method has been developed for the simultaneous d...

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