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Brexpiprazole-d8-1

Brexpiprazole-d8-1 (OPC-34712-d8-1) is the deuterium labeled 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)[3].

Product Specifications

CAS Number

1427049-19-1

Product Name Alternative

OPC-34712-d8-1

UNSPSC

12352005

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

96.48

Solubility

10 mM in DMSO

Smiles

O=C1C=CC2=CC=C(C=C2N1)OC([2H])([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])N3CCN(CC3)C4=C5C(SC=C5)=CC=C4

Molecular Formula

C25H19D8N3O2S

Molecular Weight

441.62

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.|[2]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.|[3]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

Storage Conditions

4°C (Powder, protect from light)

Scientific Category

Isotope-Labeled Compounds

Clinical Information

No Development Reported

Isoform

5-HT1 Receptor;5-HT2 Receptor

Available Sizes

Frequently Asked Questions

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