RP-5063

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

RP-5063 (Brilaroxazine) 是一种多模式多巴胺和血清素调节剂，对 DA D2、D3、D4、5-HT1A 和 5-HT2AR 具有部分激动剂活性，对 5-HT2B、5-HT6 和 5-HT7R 具有拮抗剂活性。

RP-5063 (Brilaroxazine) is a multimodal dopamine and serotonin modulator with partial agonist activity at DA D2, D3, D4, 5-HT1A, and 5-HT2ARs, and antagonist activity at 5-HT2B, 5-HT6 and 5-HT7Rs; produces dose-dependent reductions in pulmonary blood vessel wall thickness and proportion of muscular vessels, blocks MCT-induced increases in the plasma cytokines TNFα, IL-1β, and IL-6 in vivo; prevents Sugen 5416-hypoxia-induced pulmonary arterial hypertension in rats; improves declarative memory and psychosis in mouse models of schizophrenia.Schizophrenia Phase 2 Clinical.

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Brilaroxazine (oral gavage; 10 mg/kg; twice daily; 28 days) limits the functional and structural effects of pulmonary arterial hypertension (PAH), with significant improvements in pulmonary hemodynamics, right ventricular (RV) hypertrophy, SO2, and pulmonary blood vessel structural changes. Animal Model:SD-rats Dosage:10 mg/kg Administration:Oral gavage; twice daily; 28 days Result:Had the efficacy in PAH, and mitigated the functional and structural effects of MCT-induced PAH.

RP5063

GPCR/G Protein

Dopamine Receptor

Dopamine Receptor

Neurological Disease

Schizophrenia

1239729-06-6

450.36

C22H25Cl2N3O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (222.04 mM)

C1CN(CCN1CCCCOC2=CC3=C(C=C2)OCC(=O)N3)C4=C(C(=CC=C4)Cl)Cl

6-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butoxy)-2H-benzo[b][1,4]oxazin-3(4H)-one

(-20℃)

With Ice Pack

≥ 2 years