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Brexpiprazole (hydrochloride)

Brexpiprazole (OPC-34712) hydrochloride, 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 hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride 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

913612-38-1

Product Name Alternative

OPC-34712 (hydrochloride)

UNSPSC

12352005

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-hydrochloride.html

Solubility

10 mM in DMSO

Smiles

O=C1NC2=C(C=CC(OCCCCN3CCN(C4=C(C=CS5)C5=CC=C4)CC3)=C2)C=C1.[H]Cl.[x]

Molecular Formula

C25H27N3O2S.xHCl

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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

5-HT1 Receptor;5-HT2 Receptor; D2 Receptor; mLAG-3; α-1 microglobulin

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