Brexpiprazole hydrochloride

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CAS NO:

913612-38-1

OPC-34712 hydrochloride

Brexpiprazole (OPC-34712) hydrochloride，一种非典型的、具有口服活性的抗精神紊乱剂，是人5-HT1A和多巴胺受体（dopamine D_2Lreceptor）的部分激动剂，K_i分别为 0.12 nM 和 0.3 nM。Brexpiprazole hydrochloride 也是5-HT2A受体的拮抗剂，K_i为 0.47 nM。Brexpiprazole hydrochloride 对人去甲肾上腺素能受体 α_1B(K_i=0.17 nM) 和 α_2C(K_i=0.59 nM) 也显示出强效拮抗活性。

生物活性

Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic drug, is a partial agonist of human5-HT1Aanddopamine D_2LreceptorwithK_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a5-HT2Areceptor antagonist with aK_iof 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α_1B(K_i=0.17 nM) and α_2Creceptors (K_i=0.59 nM)^[1]^[2].

IC₅₀& Target

5-HT_1AReceptor

0.12 nM (Ki)

5-HT_2AReceptor

0.47 nM (Ki)

D_2LReceptor

0.3 nM (Ki)

human noradrenergic α_1B

0.17 nM (Ki)

human noradrenergic α_2C

0.59 nM (Ki)

体外研究
(In Vitro)

Brexpiprazole (0-1.0 μM, 4 days) potentiates NGF-induced neurite outgrowth in a dose-dependent manner in PC12 cells^[1].

体内研究
(In Vivo)

Brexpiprazole (0-0.1 mg/kg; p.o.; once) improves social recognition deficits in mice^[2].

Animal Model:	Male C57BL/6NCrSlc mice, Dizocilpine (0.1 mg/kg) (HY-15084B) induced social recognition deficits^[2]
Dosage:	0.01, 0.03 and 0.1 mg/kg
Administration:	Oral administration, once
Result:	Significantly ameliorated Dizocilpine-induced social recognition deficits, without sedation or a reduction of exploratory behavior.

Clinical Trial

Formula

C₂₅H₂₈ClN₃O₂S

CAS 号

913612-38-1

中文名称

盐酸依匹哌唑

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.