Epipregnanolone Explained

Epipregnanolone, also known as 3β-hydroxy-5β-pregnan-20-one, 3β,5β-tetrahydroprogesterone, or 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.

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[5] and GABAA receptors[6] and also acts as a TRPM3 channel activator.[7] [8]

Chemistry

See also: List of neurosteroids.

See also

Notes and References

  1. Book: Neurosteroids and Brain Function. 12 December 2001. Academic Press. 978-0-08-054423-6. 18–.
  2. Book: Abraham Weizman. Neuroactive Steroids in Brain Function, Behavior and Neuropsychiatric Disorders: Novel Strategies for Research and Treatment. 1 February 2008. Springer Science & Business Media. 978-1-4020-6854-6. 6–.
  3. Book: Jan Egebjerg. Arne Schousboe. Povl Krogsgaard-Larsen. Glutamate and GABA Receptors and Transporters: Structure, Function and Pharmacology. 4 October 2001. CRC Press. 978-0-7484-0881-8. 248–.
  4. Beyer. C.. González-Flores. O.. Ramı́rez-Orduña. J.M.. González-Mariscal. G.. Indomethacin Inhibits Lordosis Induced by Ring A-Reduced Progestins: Possible Role of 3α-Oxoreduction in Progestin-Facilitated Lordosis. Hormones and Behavior. 35. 1. 1999. 1–8. 0018-506X. 10.1006/hbeh.1998.1457. 10049597. 11520064 .
  5. Book: Norman G. Bowery. Allosteric Receptor Modulation in Drug Targeting. 19 June 2006. CRC Press. 978-1-4200-1618-5. 112–.
  6. Park-Chung M, Malayev A, Purdy RH, Gibbs TT, Farb DH . Sulfated and unsulfated steroids modulate gamma-aminobutyric acidA receptor function through distinct sites . Brain Res. . 830 . 1 . 72–87 . 1999 . 10350561 . 10.1016/s0006-8993(99)01381-5. 44664830 . free .
  7. Book: Issues in Pharmacology, Pharmacy, Drug Research, and Drug Innovation: 2011 Edition. 9 January 2012. ScholarlyEditions. 978-1-4649-6342-1. 3260–.
  8. Book: Advances in Glutamic Acid Research and Application: 2013 Edition: ScholarlyBrief. 21 June 2013. ScholarlyEditions. 978-1-4816-7049-4. 104–.

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