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

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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

548.97

C₂₅H₂₈D₆Cl₃N₅O₂

82752-99-6

萘法唑酮二盐酸盐-d₆；二盐酸萘法唑酮-d₆

Room temperature in continental US; may vary elsewhere.

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

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

  [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.  [Content Brief]

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