标签归档：brexpiprazole

Brexpiprazole S-oxide D8(Synonyms: DM-3411 D8)

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Brexpiprazole S-oxide D8 (Synonyms: DM-3411 D8)

Brexpiprazole S-oxide D8 (DM-3411 D8) 是 Brexpiprazole S-oxide 的氘代物。Brexpiprazole S-oxide 是 Brexpiprazole 的主要代谢产物，并通过细胞色素 P450 3A4 (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 0.12 nM 和 0.3 nM。Brexpiprazole 也是 5-HT2A 受体的拮抗剂，Ki 为 0.47 nM。

Brexpiprazole S-oxide D8(Synonyms: DM-3411 D8)

Brexpiprazole S-oxide D8 Chemical Structure

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生物活性

Brexpiprazole S-oxide D8 (DM-3411 D8) is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide 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].

IC50 & Target[2]

5-HT1A Receptor

0.12 nM (Ki)

5-HT2A Receptor

0.47 nM (Ki)

D2 Receptor

0.3 nM (Ki)

分子量

457.61

Formula

C25H19D8N3O3S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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