Brilaroxazine (RP5603) 是一种有效的具有口服活性的多巴胺/5-羟色胺 (dopamine (DA)/5-HT) 调节剂。Brilaroxazine 是多巴胺 (DA) D2，D3 和 D4 受体，血清素 5-HT1A (Ki=1.5 nM) 和 5-HT2A (Ki=2.5 nM) 的部分激动剂，对 5-HT2B (Ki=0.19 nM) 和 5-HT7?(Ki=2.7 nM) 受体具有拮抗剂活性。Brilaroxazine 是一种非典型抗精神病试剂，在动物模型中，具有改善神经精神病和神经疾病的认知障碍的潜力。
货号:ajcx38078
CAS:1239729-06-6
分子式:C22H25Cl2N3O3
分子量：450.36
溶解度:DMSO : 100 mg/mL (222.04 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

[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 model.Eur J Pharmacol. 2018 May 15;827:159-166.
[3]. L. Bhat,et al. Rp5063 Prevents Monocrotaline Induced Pulmonary Arterial Hypertension In Rats.