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伊潘立酮, 羟色胺 2a(5-HT2a)受体拮抗剂

5-HT Receptor Inhibitors
  • CAS编号: 133454-47-4
  • 分子式: C24H27FN2O4
  • 分子量: 426.48
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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
I408549-1ml
1ml 现货 Stock Image
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Compound libraries (12333)

基本描述

英文别名 HP873 | 1-(4-(3-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)propoxy)-3-methoxyphenyl)ethanone
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Iloperidone
生化机理 伊洛哌酮(HP873)是一种多巴胺(D2)/羟色胺(5-HT2)受体拮抗剂,用于治疗精神分裂症。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 拮抗剂
作用机制 羟色胺 2a(5-HT2a)受体拮抗剂
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

Information

Iloperidone Iloperidone (HP873) is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.
In vitro

Iloperidone displays high affinity (Ki < 10 nM) for norepinephrine alpha(1)-adrenoceptors, dopamine D(3) and serotonin 5-HT(2A) receptors. Iloperidone displays higher affinity for the dopamine D3 receptor (Ki = 7.1 nM) than for the dopamine D4 receptor (Ki = 25 nM). Iloperidone displays high affinity for the 5-HT6 and 5-HT7 receptors (Ki = 42.7 nM and 21.6 nM, respectively), and is found to have higher affinity for the 5-HT2A (Ki = 5.6 nM) than for the 5-HT2C receptor (Ki = 42.8 nM). Iloperidone significantly increases dopa accumulation, an index of dopamine turnover in response to D2 receptor blockade, at doses from 0.3 mg/kg to 10 mg/kg i.p. in the striatum and from 1 mg/kg to 10 mg/kg in the nucleus accumbens.

In vivo

Iloperidone exerts behavioral effects in pharmacological rats models of disrupted sensorimotor gating consistent with "atypical" antipsychotics, mediated by antagonism of dopaminergic and noradrenergic receptors. Iloperidone (1 and 3 mg/kg) prevents the PPI-disruptive effects of treatment with 1 mg/kg PCP. Iloperidone (0.3 mg/kg) prevents cirazoline-induced PPI deficits, independent of its effects on startle magnitude. Iloperidone (10 mg/kg) and Melperone (10 mg/kg) produce an equivalent or a smaller increase in DA release in the nucleus accumbens (NAC) of rats, respectively, compared to the mPFC, whereas none of them increase acetylcholine (ACh) release in the NAC.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥99%

产品属性

ALogP 4.1

关联靶点(人)

DRD2 Tclin D(2)多巴胺受体(D(2) dopamine receptor) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
SIGMAR1 Tclin Sigma 非阿片类细胞内受体 1(Sigma non-opioid intracellular receptor 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HTR7 Tclin 5-羟色胺受体 7(5-hydroxytryptamine receptor 7) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HTR1A Tclin 5-羟色胺受体 1A(5-hydroxytryptamine receptor 1A) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HTR6 Tchem 5-羟色胺受体 6(5-hydroxytryptamine receptor 6) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Isomeric SMILES CC(=O)C1=CC(=C(C=C1)OCCCN2CCC(CC2)C3=NOC4=C3C=CC(=C4)F)OC
分子量 426.48
Reaxy-Rn 7233425
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7233425&ln=

化学和物理性质

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
信号词 Danger
危险声明

H300: 吞咽致命

预防措施声明

P321: 特殊处理(请参阅此标签上的...)。

P405: 密闭存放

P501: 将内容物/容器处理到。。。

P264: 处理后要彻底洗手。

P270: 使用本产品时,请勿进食、饮水或吸烟。

P330: 漱口

P301+P316: 如果吞咽:立即寻求紧急医疗救助。

WGK Germany 1
RTECS KM5777850
Merck Index 4900

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