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伊潘立酮

规格或纯度: ≥98%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
I125279-50mg
50mg 现货 Stock Image
I125279-250mg
250mg 现货 Stock Image
I125279-1g
1g 现货 Stock Image
I125279-5g
5g 期货 Stock Image

基本描述

规格或纯度 ≥98%
英文名称 Iloperidone
别名 伊潘立酮
英文别名 Iloperidone|133454-47-4|Fanapt|Zomaril|Fanapta|HP 873|HP-873|Iloperidone (Fanapt)|iloperidona|iloperidonum|4'-(3-(4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidino)propoxy)-3'-methoxyacetophenone|UNII-VPO7KJ050N|1-[4-[3-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperid
生化机理 Iloperidone is an atypical antipsychotic, a combined dopamine (D2) and serotonin (5HT2) receptor antagonist. Iloperidone targets a selective set of dopamine, serotonin and also norepinephrine receptor subtypes. Like similar atypical antipsychotics, Iloperidone has higher affinity for the 5-HT2A receptor (Ki < 10 nM) than for the D2 receptor (Ki = 10–100) nM). Iloperidone has high affinity for dopamine D3 (Ki < 10 nM) and lower affinity for other serotonin or dopamine subtypes. Unlike most atypical antipsychotics, Iloperidone also has high affinity for norepinephrine alpha1 receptors (Ki < 10 nM) which may contribute to the drμg’s efficacy on mood and cognition.
应用 A dopamine (D2) and serotonin (5HT2) receptor antagonist
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 250mg卖完停产,不再备货
产品介绍

Iloperidone (伊潘立酮; HP 873) 是D2/5-HT2受体拮抗剂,可作用于精神分裂症。A dopamine (D2) and serotonin (5HT2) receptor antagonist

Iloperidone is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.
A dopamine (D2) and serotonin (5HT2) receptor antagonist

名称和标识符

IUPAC Name 1-[4-[3-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]propoxy]-3-methoxyphenyl]ethanone
INCHI InChI=1S/C24H27FN2O4/c1-16(28)18-4-7-21(23(14-18)29-2)30-13-3-10-27-11-8-17(9-12-27)24-20-6-5-19(25)15-22(20)31-26-24/h4-7,14-15,17H,3,8-13H2,1-2H3
InChi Key XMXHEBAFVSFQEX-UHFFFAOYSA-N
Canonical SMILES CC(=O)C1=CC(=C(C=C1)OCCCN2CCC(CC2)C3=NOC4=C3C=CC(=C4)F)OC
WGK Germany 1
RTECS KM5777850
PubChem CID 71360
分子量 426.48
Reaxy-Rn 7233425

化学和物理性质

溶解性 DMSO 27 mg/mL Water <1 mg/mL Ethanol 4 mg/mL
敏感性 对热敏感
闪点(℉) 48.2?°F
闪点(℃) 48.2°F
熔点 118-120°C

安全和危险性(GHS)

象形图
ghs06

Toxic

信号词 Danger
危险声明 H300: Fatal if swallowed
预防措施声明 P321,P405,P501,P264,P270,P330,P301+P316
WGK Germany 1
RTECS KM5777850
Reaxy-Rn 7233425
Merck Index 4900

关联配体

Ligand ID 87
名称 iloperidone
别名 Fanapt®
类别 Synthetic organic
学名 1-[4-[3-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]propoxy]-3-methoxyphenyl]ethanone
生物活性评价 Measuring displacement of [3H]spiperone from rat cortex provides an IC50 value for iloperidone of 9nM . The ratio of IC50 values of dopamine D2 binding over 5-HT2 binding is 12.2. When >1, this ratio indicates the potential efficacy of a drug as an atypical antipsychotic .
We have been unable to find open-access data for iloperidone at the human dopamine D2 and serotonin 5-HT2 receptors to substantiate the drug's MMOA.
评价 Iloperidone is an atypical antipsychotic drug.

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参考文献

1. Meltzer HY, Matsubara S, Lee JC.  (1989)  The ratios of serotonin2 and dopamine2 affinities differentiate atypical and typical antipsychotic drugs..  Psychopharmacol Bull,  25  (3):  (390-2).  [PMID:2576319]
2. Strupczewski JT, Bordeau KJ, Chiang Y, Glamkowski EJ, Conway PG, Corbett R, Hartman HB, Szewczak MR, Wilmot CA, Helsley GC.  (1995)  3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873)..  J Med Chem,  38  (7):  (1119-31).  [PMID:7707315]

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品牌简介

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