| Bioactivity | 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 (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors[1]. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo[2]. |
| 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[1]. Animal Model: |
| Name | Brilaroxazine |
| CAS | 1239729-06-6 |
| Formula | C22H25Cl2N3O3 |
| Molar Mass | 450.36 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [1]. Reviva Pharmaceuticals Reports RP5063 Positive Efficacy Results for Memory Deficits [2]. Bhat L, et al. Evaluation of the effects of RP5063, a novel, multimodal, serotonin receptor modulator, as single-agent therapy and co-administrated with sildenafil, bosentan, and treprostinil in a monocrotaline-induced pulmonary arterial hypertension rat [3]. L. Bhat,et al. Rp5063 Prevents Monocrotaline Induced Pulmonary Arterial Hypertension In Rats. |
Brilaroxazine
CAS: 1239729-06-6 F: C22H25Cl2N3O3 W: 450.36
Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine
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