Diphendramine-d6 (drochloride) is the deuterium labeled Diphendramine drochloride. Diphendramine drochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphendramine drochloride can across the ovine blood-brain barrier (BBB)[1][2].
Stable heavy isotopes of drogen, 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]. Simons FE. H1-receptor antagonists. Comparative tolerability and safety. Drug Saf. 1994;10(5):350-380.
[3]. Sadiq MW, et al. Diphendramine active uptake at the blood-brain barrier and its interaction with oxycodone in vitro and in vivo. J Pharm Sci. 2011;100(9):3912-3923.