Brexpiprazole-d8-1

Modify Date: 2024-01-30 00:58:29

Brexpiprazole-d8-1 Structure
Brexpiprazole-d8-1 structure
Common Name Brexpiprazole-d8-1
CAS Number 1427049-19-1 Molecular Weight 441.62
Density N/A Boiling Point N/A
Molecular Formula C25H19D8N3O2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Brexpiprazole-d8-1


Brexpiprazole-d8-1 is the deuterium labeled Brexpiprazole[1]. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic drug, 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].

 Names

Name Brexpiprazole-d8-1

 Brexpiprazole-d8-1 Biological Activity

Description Brexpiprazole-d8-1 is the deuterium labeled Brexpiprazole[1]. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic drug, 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].
Related Catalog
In Vitro Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
References

[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.  

 Chemical & Physical Properties

Molecular Formula C25H19D8N3O2S
Molecular Weight 441.62