Brexpiprazole-d8-1

Brexpiprazole-d8-1

• CAS Number: 1427049-19-1
• UNSPSC Description: Brexpiprazole-d8-1 is the deuterium labeled Brexpiprazole[1]. 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].
• Target Antigen: 5-HT Receptor; Adrenergic Receptor; Dopamine Receptor
• Type: Isotope-Labeled Compounds
• Related Pathways: GPCR/G Protein;Neuronal Signaling
• Applications: Neuroscience-Neuromodulation
• Field of Research: Neurological Disease
• 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 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
• Clinical Information: No Development Reported