1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
    5-HT Receptor
  3. Brilaroxazine

Brilaroxazine (Synonyms: RP5063)

Cat. No.: HY-109112
Handling Instructions

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.

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Brilaroxazine Chemical Structure

Brilaroxazine Chemical Structure

CAS No. : 1239729-06-6

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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[1]. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo[2].

IC50 & Target[1][2]

5-HT1A Receptor

1.5 nM (Ki)

5-HT2A Receptor

2.5 nM (Ki)

5-HT2B Receptor

0.19 nM (Ki)

5-HT7 Receptor

2.7 nM (Ki)

D2 Receptor

 

D3 Receptor

 

D4 Receptor

 

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: SD-rats[2]
Dosage: 10 mg/kg
Administration: Oral gavage; twice daily; 28 days
Result: Had the efficacy in PAH, and mitigated the functional and structural effects of MCT-induced PAH.
Molecular Weight

450.36

Formula

C₂₂H₂₅Cl₂N₃O₃

CAS No.

1239729-06-6

SMILES

O=C1NC2=CC(OCCCCN3CCN(C(C=CC=C4Cl)=C4Cl)CC3)=CC=C2OC1

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

BrilaroxazineRP5063RP 5063RP-5063Dopamine Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorPulmonaryarterialhypertensionPAHdepressivedisorder,Tourettesyndrome,ADHD AlzheimerParkinsonautismcardiacInhibitorinhibitorinhibit

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Brilaroxazine
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