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Brilaroxazine (RP5063) is a potent multimodal dopamine/5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $107 | In Stock | |
5 mg | $263 | In Stock | |
10 mg | $428 | In Stock | |
25 mg | $737 | In Stock | |
50 mg | $1,060 | In Stock | |
100 mg | $1,450 | In Stock | |
500 mg | $2,880 | In Stock | |
1 mL x 10 mM (in DMSO) | $387 | In Stock |
Description | Brilaroxazine (RP5063) is a potent multimodal dopamine/5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases. |
Targets&IC50 | 5-HT2B receptor:0.19 nM (Ki), 5-HT2A receptor:2.5 nM (Ki), 5-HT7 receptor:2.7 nM (Ki), 5-HT1A receptor:1.5 nM (Ki) |
In vivo | Brilaroxazine (10 mg/kg) had efficacy in PAH, and mitigated the functional and structural effects of MCT-induced PAH, with significant improvements in pulmonary hemodynamics, right ventricular (RV) hypertrophy, SO2, and pulmonary blood vessel structural changes[3]. |
Alias | RP5063 |
Molecular Weight | 450.36 |
Formula | C22H25Cl2N3O3 |
Cas No. | 1239729-06-6 |
Smiles | Clc1cccc(N2CCN(CCCCOc3ccc4OCC(=O)Nc4c3)CC2)c1Cl |
Relative Density. | 1.301 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 95 mg/mL (210.94 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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