Brexpiprazole-d8

Brexpiprazole-d8 (OPC-34712-d8) is the deuterium labeled Brexpiprazole (HY-15780) . 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) [2][3].

Product Specifications

CAS Number

[1427049-21-5]

Product Name Alternative

OPC-34712-d8

UNSPSC

12352005

Hazard Statement

H302, H400, H410

Target

5-HT Receptor; Adrenergic Receptor; Dopamine Receptor; Isotope-Labeled Compounds

Type

Isotope-Labeled Compounds

Related Pathways

GPCR/G Protein; Neuronal Signaling; Others

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Purity

99.90

Solubility

10 mM in DMSO

Smiles

O=C1NC2=C(C=CC(OCCCCN3C([2H])([2H])C([2H])([2H])N(C4=C(C=CS5)C5=CC=C4)C([2H])([2H])C3([2H])[2H])=C2)C=C1

Molecular Formula

C25H19D8N3O2S

Molecular Weight

441.62

Precautions

H302, H400, H410

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.