Nefazodone-d6 dihydrochloride(Synonyms: BMY-13754-d6 dihydrochloride; MJ-13754-1-d6 dihydrochloride)

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Nefazodone-d6 dihydrochloride (Synonyms: BMY-13754-d6 dihydrochloride; MJ-13754-1-d6 dihydrochloride)

Nefazodone-d6 (dihydrochloride) 是 Nefazodone (hydrochloride) 氘代物。Nefazodone hydrochloride (BMY-13754) 是一种强效和选择性的 5HT2A (Ki=5.8 nM) 拮抗剂，对 5-HT 和去甲肾上腺素摄取具有中度抑制作用 (IC50 分别为 290 和 300 nM)。Nefazodone hydrochloride 是一种苯哌嗪类抗抑郁药，具有微弱的 α-肾上腺素阻断活性。

Nefazodone-d6 dihydrochloride(Synonyms: BMY-13754-d6 dihydrochloride; MJ-13754-1-d6 dihydrochloride)

Nefazodone-d6 dihydrochloride Chemical Structure

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生物活性

Nefazodone-d6 (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

548.97

Formula

C25H28D6Cl3N5O2
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Pullar IA, et al. LY367265, an inhibitor of the 5-hydroxytryptamine transporter and 5-hydroxytryptamine(2A) receptor antagonist: a comparison with the antidepressant, nefazodone. Eur J Pharmacol. 2000;407(1-2):39-46.

    [3]. Ellingrod VL, et al. Nefazodone: a new antidepressant. Am J Health Syst Pharm. 1995;52(24):2799-2812.

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