1'-Hydroxymidazolam-d4

1'-Hydroxymidazolam-d4 is the deuterium labeled 1'-Hydroxymidazolam. 1'-Hydroxymidazolam is a primary active metabolite of Midazolam, and it is a neuronal depressant agent. 1'-Hydroxymidazolam could inhibit neuronal activity add to the effects of Midazolam[1][2].

Signaling Pathways >> Others >> Others

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[3].

[1]. Hasegawa T, et, al. Increase in the systemic exposure of primary metabolites of Midazolam in rat arising from CYP inhibition or hepatic dysfunction. Drug Metab Pharmacokinet. 2017 Feb; 32(1): 69-76.  

[2]. Balk M, et, al. Differential depression of neuronal network activity by midazolam and its main metabolite 1-hydroxymidazolam in cultured neocortical slices. Sci Rep. 2017 Jun 14; 7(1): 3503.  

[3]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223.