5β-Pregnan-3α-ol-20-one-17α,21,21,21-d4

5β-Pregnan-3α-ol-20-one-17α,21,21,21-d4 is the deuterium labeled Pregnanolone. Pregnanolone (Eltanolone), a Progesterone metabolite, is a neurosteroid. Pregnanolone is a GABAA receptor positive allosteric modulator. Pregnanolone has anxiolytic and antidepressant effects[1].

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> GABA Receptor

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]. Tereza Smejkalova, et al. Endogenous neurosteroids pregnanolone and pregnanolone sulfate potentiate presynaptic glutamate release through distinct mechanisms. Br J Pharmacol. 2021 Oct;178(19):3888-3904.