Desvenlafaxine-d10

Modify Date: 2024-01-09 19:58:00

Desvenlafaxine-d10 Structure
Desvenlafaxine-d10 structure
Common Name Desvenlafaxine-d10
CAS Number 1062607-49-1 Molecular Weight 273.44
Density 1.1±0.1 g/cm3 Boiling Point 403.8±25.0 °C at 760 mmHg
Molecular Formula C16H15D10NO2 Melting Point N/A
MSDS N/A Flash Point 193.2±21.8 °C

 Use of Desvenlafaxine-d10


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].

 Names

Name 4-{2-(Dimethylamino)-1-[1-hydroxy(2H10)cyclohexyl]ethyl}phenol
Synonym More Synonyms

 Desvenlafaxine-d10 Biological Activity

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
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.

 Chemical & Physical Properties

Density 1.1±0.1 g/cm3
Boiling Point 403.8±25.0 °C at 760 mmHg
Molecular Formula C16H15D10NO2
Molecular Weight 273.44
Flash Point 193.2±21.8 °C
Exact Mass 273.251312
LogP 2.26
Vapour Pressure 0.0±1.0 mmHg at 25°C
Index of Refraction 1.573

 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