Lofexidine-d4 hydrochloride

Lofexidine-d4 hydrochloride (Baq-168-d4) is the deuterium labeled Lofexidine hydrochloride. Lofexidine hydrochloride is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal[1][2].

Research Areas >> Endocrinology

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Neurological Disease

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].

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

[2]. Vartak AP, et al. The preclinical discovery of lofexidine for the treatment of opiate addiction. Expert Opin Drug Discov. 2014 Nov;9(11):1371-7.

[3]. Gish EC, et al. Lofexidine, an {alpha}2-receptor agonist for opioid detoxification. Ann Pharmacother. 2010 Feb;44(2):343-51.