Nefazodon-d4 (hydrochloride)

Nefazodone-d4 (hydrochloride) (BMY-13754-d4) 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].

BMY-13754-d4; MJ-13754-1-d4

12352211

5-HT Receptor; Adrenergic Receptor; Isotope-Labeled Compounds

GPCR/G Protein; Neuronal Signaling; Others

Metabolism-protein/nucleotide metabolism

Neurological Disease; Endocrinology

O=C1N(CCCN2CCN(C3=C([2H])C([2H])=C([2H])C(Cl)=C3[2H])CC2)N=C(CC)N1CCOC4=CC=CC=C4.Cl

C25H29D4Cl2N5O2

510.49

[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.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-B1396S3/

Isotope-Labeled Compounds

No Development Reported

5-HT2 Receptor