1062607-49-1

1062607-49-1 structure

Name: Desvenlafaxine-d10
Chemical Name: 4-{2-(Dimethylamino)-1-[1-hydroxy(2H10)cyclohexyl]ethyl}phenol
CAS Number: 1062607-49-1
Molecular Formula: C₁₆H₁₅D₁₀NO₂
Molecular Weight: 273.44
Catalog: Signaling Pathways Neuronal Signaling Serotonin Transporter
Create Date: 2018-06-05 00:45:17
Modify Date: 2024-01-09 19:58:00
Desvenlafaxine-d10 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].

Name	4-{2-(Dimethylamino)-1-[1-hydroxy(2H10)cyclohexyl]ethyl}phenol
Synonyms	Phenol, 4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl-2,2,3,3,4,4,5,5,6,6-d10)ethyl]- 4-{2-(Dimethylamino)-1-[1-hydroxy(2H10)cyclohexyl]ethyl}phenol

Description	Desvenlafaxine-d10 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> Neuronal Signaling >> Serotonin Transporter
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].
References	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Deecher, D.C., et al., Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther, 2006. 318(2): p. 657-65. [3]. Sopko, M.A., Jr., M.J. Ehret, and M. Grgas, Desvenlafaxine: another "me too" drug? Ann Pharmacother, 2008. 42(10): p. 1439-46.