Brexpiprazole S-oxide

BrexpiprazoleS-oxide(DM-3411)是Brexpiprazole的主要代谢产物，并通过细胞色素P4503A4(CYP3A4)代谢。Brexpiprazole是一种非典型抗精神病药，是人5-HT1A和多巴胺受体的部分激动剂，Ki分别为0.12nM和0.3nM。Brexpiprazole也是5-HT2A受体的拮抗剂，Ki为0.47nM。

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Background

Brexpiprazole S-oxide (DM-3411) is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine 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[1][2][3].

[1]. Chen B, et al. Effects of 26 Recombinant CYP3A4 Variants on Brexpiprazole Metabolism. Chem Res Toxicol. 2019 Oct 17. [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.