Iloperidone hydrochloride

立即咨询

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。

CAS NO:

1299470-39-5

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

盐酸伊潘立酮
HP 873 hydrochloride

产品介绍

Iloperidone hydrochloride (HP 873 hydrochloride) 是一种D₂/5-HT₂受体拮抗剂，可作用于精神分裂症的非典型抗精神病药。

生物活性

Iloperidone hydrochloride (HP 873 hydrochloride) is aD₂/5-HT₂receptor antagonist. Iloperidone hydrochloride is an atypical antipsychotic for the schizophrenia symptoms^[1]^[2].

IC₅₀& Target^[1]

Rat D₂Receptor

54 nM (Ki)

Rat 5-HT₂Receptor

3.1 nM (Ki)

Rat D₁Receptor

546 nM (Ki)

Rat 5-HT_1AReceptor

168 nM (Ki)

Rat 5-HT₆Receptor

42.7 nM (Ki)

Rat 5-HT₇Receptor

21.6 nM (Ki)

Human D₁Receptor

216 nM (Ki)

Human D₃Receptor

7.1 nM (Ki)

Human D₄Receptor

25 nM (Ki)

Human D₅Receptor

319 nM (Ki)

Human 5-HT_2AReceptor

5.6 nM (Ki)

Human 5-HT_2CReceptor

42.8 nM (Ki)

体外研究
(In Vitro)

Iloperidone hydrochloride displays higher affinity for the dopamine D₃receptor (K_i=7.1 nM) than for the dopamine D₄receptor (K_i=25 nM). Iloperidone displays high affinity for the 5-HT₆and 5-HT₇receptors (K_i=42.7 and 21.6 nM, respectively), and is found to have higher affinity for the 5-HT_2A(Ki=5.6 nM) than for the 5-HT_2Creceptor (K_i=42.8 nM)^[1].

体内研究
(In Vivo)

Iloperidone hydrochloride is eliminated slowly, with a mean t_1/2of 13.5 to 14.0 hours. Coadministration with food did not significantly affect AUC, t_max, or C_max. These results indicate that the rate of iloperidone's absorption is decreased, but the overall bioavailability is unchanged, when the drug is taken with food. Orthostatic hypotension, dizziness, and somnolence were the most commonly reported adverse events^[2].

Clinical Trial

分子量

462.94

Formula

C₂₄H₂₈ClFN₂O₄

CAS 号

1299470-39-5

中文名称

盐酸伊潘立酮；盐酸哌啶酮

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.