Description
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. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.
Product information
CAS Number: 1239729-06-6
Molecular Weight: 450.36
Formula: C22H25Cl2N3O3
Synonym:
RP5063
Chemical Name: 6-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-3,4-dihydro-2H-1,4-benzoxazin-3-one
Smiles: O=C1COC2=CC=C(C=C2N1)OCCCCN1CCN(CC1)C1=CC=CC(Cl)=C1Cl
InChiKey: PMKMNTBZJOXTJW-UHFFFAOYSA-N
InChi: InChI=1S/C22H25Cl2N3O3/c23-17-4-3-5-19(22(17)24)27-11-9-26(10-12-27)8-1-2-13-29-16-6-7-20-18(14-16)25-21(28)15-30-20/h3-7,14H,1-2,8-13,15H2,(H,25,28)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
References:
- Reviva Pharmaceuticals Reports RP5063 Positive Efficacy Results for Memory Deficits
- 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.
- L. Bhat,et al. Rp5063 Prevents Monocrotaline Induced Pulmonary Arterial Hypertension In Rats.
Products are for research use only. Not for human use.
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