Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A ( K i =1.5 nM) and 5-HT2A ( K i =2.5 nM), and has antagonist activity at 5-HT2B ( K i =0.19 nM), and 5-HT7 ( K i =2.7 nM) receptors Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo . In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SD-ratsDosage: 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. Form:Solid IC50& Target:5-HT|1A|Receptor|1.5 nM (Ki)|5-HT|2A|Receptor|2.5 nM (Ki)|5-HT|2B|Receptor|0.19 nM (Ki)|5-HT|7|Receptor|2.7 nM (Ki)|D|2|Receptor|D|3|Receptor|D|4|Receptor
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Brilaroxazine
CAS number:1239729-06-6 molecular formula:C22H25Cl2N3O3
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| Chinese alias | 布拉罗嗪 | ||
| English alias | MS-28159 | 2036070-48-9 | UNII-X8L60BA01I | Brilaroxazine | 6-(4-(4-(2,3-Dichlorophenyl)-piperazin-1-yl)-butoxy)-2H-benzo(b)(1,4)oxazin-3(4H)-one | 6-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butoxy)-2H-benzo(b)(1,4)oxazin-3(4H)-one | 2H-1,4-Benzoxazin-3(4 | ||
| CAS number | 1239729-06-6 | molecular formula | C22H25Cl2N3O3 |
| molecular weight | 450.36 g/mol | Exact mass | ≥98% |
| PSA | 54.000 Ų | logp | 4.400 |
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