1. APIs
  2. Nestorone
  3. Nestorone Metabolites
  4. 5α-dihydronestorone

5α-dihydronestorone

Structure

Notes

Identified in vitro, detected in plasma and brain of mice. Most abundant metabolite in mouse brain at 30 min post administration. 17 times less potent PR activity than nestorone in human PR transactivation assay (EC50 = 410 pM vs. EC50 of Nestorone = 24 pM).

References

  1. Kumar, N.; Fagart, J.; Liere, P.; Mitchell, S. J.; Knibb, A. R.; Petit-Topin, I.; Rame, M.; El-Etr, M.; Schumacher, M.; Lambert, J. J.; Rafestin-Oblin, M. E.; Sitruk-Ware, R., Nestorone(R) as a Novel Progestin for Nonoral Contraception: Structure-Activity Relationships and Brain Metabolism Studies. Endocrinology 2017, 158 (1), 170-182.
    2. (View all citations for this reference)