Brilaroxazine

SKU: orb1308521

Description

Brilaroxazine (RP5063) is a multimodal dopamine and serotonin modulator, acting as a partial agonist at D2, D3, D4, 5-HT1A, and 5-HT2A receptors and an antagonist at 5-HT2B and 5-HT7 receptors. Its pharmacological profile supports research into cognitive deficits associated with schizophrenia and Parkinson's disease, as evidenced in preclinical in vivo models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1239729-06-6
• MW: 450.36
• Purity: 99.36% (May vary between batches)
• Formula: C₂₂H₂₅Cl₂N₃O₃
• SMILES: Clc1cccc(N2CCN(CCCCOc3ccc4OCC(=O)Nc4c3)CC2)c1Cl
• Target: Dopamine Receptor,5-HT Receptor
• Solubility: DMSO:95 mg/mL (210.94 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.33 mM)

Bioactivity

• Target IC50:
  5-HT1A receptor:1.5 nM (Ki)|5-HT7 receptor:2.7 nM (Ki)|5-HT2A receptor:2.5 nM (Ki)|5-HT2B receptor:0.19 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

syndrome,ADHD, RP5063, RP-5063, RP 5063, Pulmonary, Serotonin Receptor, 5-HT7 Receptor, 5-HT7, 5HT Receptor, 5-hydroxytryptamine Receptor, 5HTReceptor, Alzheimer, 5-HT1A Receptor, 5-HT2B Receptor, 5-HT2A Receptor, 5-HT2B, 5-HT2A, 5-HT1A, 5-HT Receptor, autism, arterial, cardiac, DopamineReceptor, Dopamine Receptor, disorder,Tourette, depressive, D4 receptor, D4 Receptor, D2 receptor, D2 Receptor, D3 Receptor, D3 receptor, Brilaroxazine, Inhibitor, hypertension, inhibit, PAH, Parkinson

Compound Identifiers

PubChem CID

46861612