PMID: 9182866Jan 1, 1997Paper

5alpha-reduction of norethisterone enhances its binding affinity for androgen receptors but diminishes its androgenic potency

The Journal of Steroid Biochemistry and Molecular Biology
A E LemusG Perez-Palacios

Abstract

Norethisterone (NET), a 19-nor synthetic progestin, undergoes enzyme-mediated 5alpha-reduction and exerts potent androgenic effects in target organs. To investigate its mode of androgenic action we examined, in a comparative manner, the in vitro metabolism of NET and testosterone (T), as well as the binding affinities to androgen receptors (AR) and the androgenic potency of NET, T, and their 5alpha-reduced derivatives. Bioconversion of [3H]-NET and [3H]-T was studied in rat prostate homogenates, AR binding affinity was assessed in rat ventral prostates using [3H]-mibolerone as the radioligand, and the androgenic potency was evaluated by the increase of beta-glucuronidase activity in the mouse kidney, and by the growth of accessory sex organs in castrated male rats. The results demonstrated that 5alpha-NET displayed a higher AR binding affinity but a significantly lower androgenic potency than unchanged NET. The bioconversion studies indicated that the metabolism of NET was similar to that of T, although to a lesser extent, thus ruling out the possibility that the synthetic progestin metabolizes rapidly into less active derivatives. To investigate the nature of the paradoxical effect of 5alpha-reduction upon the NET molecule, th...Continue Reading

References

Nov 1, 1990·Pharmacology, Biochemistry, and Behavior·G MoralíG Pérez-Palacios
Jan 1, 1985·Journal of Steroid Biochemistry·B A ChávezG Pérez-Palacios
Jun 1, 1972·Journal of Steroid Biochemistry·W G StillwellR N Stillwell
Mar 1, 1993·Molecular Reproduction and Development·R Gutiérrez-SagalM A Cerbón
Nov 1, 1959·The Journal of Clinical Endocrinology and Metabolism·M M GRUMBACHR E MOLOSHOK

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Citations

Sep 5, 2003·European Journal of Pharmacology·Mercedes PerusquíaAna E Lemus
Sep 6, 2002·Pharmacology, Biochemistry, and Behavior·G MoralíG Pérez-Palacios
Feb 19, 2003·The Journal of Steroid Biochemistry and Molecular Biology·Carlos Kubli-GarfiasFernando Larrea
Feb 19, 2003·The Journal of Steroid Biochemistry and Molecular Biology·Rocio García-BecerraFernando Larrea
Jul 23, 1999·Annals of the New York Academy of Sciences·H L BradlowJ J Byrne
Aug 28, 2004·Expert Opinion on Investigational Drugs·Melanie Walton, Richard A Anderson
Feb 28, 2002·Expert Opinion on Investigational Drugs·Brian M Brady, Richard A Anderson
Jun 25, 2016·Journal of Molecular Endocrinology·Silvia GiattiMarzia Pesaresi
Apr 19, 2012·Journal of the American Chemical Society·Paul M LevineKent Kirshenbaum
Dec 6, 2002·Endocrine Reviews·R A Anderson, D T Baird
Nov 15, 2011·Current Biology : CB·Gregory NachtrabKenneth D Poss

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