Brexpiprazole

Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) [1][2].

Product Specifications

CAS Number

[913611-97-9]

Product Name Alternative

OPC-34712

UNSPSC

12352005

Hazard Statement

H317, H319, H335

Target

5-HT Receptor; Adrenergic Receptor; Dopamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Brexpiprazole.html

Concentration

10mM

Purity

99.80

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 80°C)

Smiles

O=C1NC2=C(C=CC(OCCCCN3CCN(C4=C(C=CS5)C5=CC=C4)CC3)=C2)C=C1

Molecular Formula

C25H27N3O2S

Molecular Weight

433.57

Precautions

H317, H319, H335

References & Citations

[1]Ishima T, et al. Potentiation of neurite outgrowth by brexpiprazole, a novel serotonin-dopamine activity modulator: a role for serotonin 5-HT1A and 5-HT2A receptors. Eur Neuropsychopharmacol. 2015 Apr;25 (4) :505-11.|[2]Yoshimi N, et al. Improvement of dizocilpine-induced social recognition deficits in mice by brexpiprazole, a novel serotonin-dopamine activity modulator. Eur Neuropsychopharmacol. 2015 Mar;25 (3) :356-64.