Epipregnanolone

Epipregnanolone


Epipregnanolone, also known as 3β-Hydoxy-5β-pregnan-20-one or 3β,5β-tetrahydroprogesterone (3β,5β-THP), is an endogenous neurosteroid.[1] It acts as a negative allosteric modulator of the GABAA receptor and reverses the effects of potentiators like allopregnanolone.[2][3] Epipregnanolone is biosynthesized from progesterone by the actions of 5β-reductase and 3β-hydroxysteroid dehydrogenase, with 5β-dihydroprogesterone as the intermediate in this two-step transformation.[2]

Epipregnanolone is not a progestogen itself, but via metabolization into other steroids, behaves indirectly as one.[4]

The sulfate of epipreganolone, epipregnanolone sulfate, is a negative allosteric modulator of the NMDA receptor,[5] and also acts as a TRPM3 channel activator.[6][7]

See also

References