Relative binding affinity of anabolic-androgenic steroids: comparison of the binding to the androgen receptors in skeletal muscle and in prostate, as well as to sex hormone-binding globulin

Endocrinology
T SaartokJ A Gustafsson

Abstract

It is unclear whether anabolic steroids act on skeletal muscle via the androgen receptor (AR) in this tissue, or whether there is a separate anabolic receptor. When several anabolic steroids were tested as competitors for the binding of [3H]methyltrienolone (MT; 17 beta-hydroxy-17 alpha-methyl-4,9,11-estratrien-3-one) to the AR in rat and rabbit skeletal muscle and rat prostate, respectively, MT itself was the most efficient competitor. 1 alpha-Methyl-5 alpha-dihydrotestosterone (1 alpha-methyl-DHT; mesterolone) bound most avidly to sex hormone-binding globulin (SHBG) [relative binding affinity (RBA) about 4 times that of DHT]. Some anabolic-androgenic steroids bound strongly to the AR in skeletal muscle and prostate [ RBAs relative to that of MT: MT greater than 19-nortestosterone ( NorT ; nandrolone) greater than methenolone (17 beta-hydroxy-1-methyl-5 alpha-androst-1-en-3-one) greater than testosterone (T) greater than 1 alpha-methyl-DHT]. In other cases, AR binding was weak (RBA values less than 0.05): stanozolol (17 alpha-methyl-5 alpha- androstano [3,2-c]pyrazol-17 beta-ol), methanedienone (17 beta-hydroxy-17 alpha-methyl-1,4-androstadien-3-one), and fluoxymesterolone (9 alpha-fluoro-11 beta-hydroxy-17 alpha-methyl-T). Ot...Continue Reading

Citations

Nov 1, 1987·Pflügers Archiv : European journal of physiology·S Egginton
Jan 1, 1994·European Journal of Applied Physiology and Occupational Physiology·K InoueE Sugimoto
Feb 1, 1997·Endocrine·A M AzzaroloD W Warren
Jan 1, 1987·Journal of Steroid Biochemistry·T OjasooJ P Raynaud
Nov 1, 1994·Physiology & Behavior·A S Clark, D M Barber
Jan 1, 1989·Comparative Biochemistry and Physiology. B, Comparative Biochemistry·G BoissonneaultR R Tremblay
Oct 1, 1992·The Journal of Steroid Biochemistry and Molecular Biology·F Celotti, P Negri Cesi
Oct 1, 1994·The Journal of Steroid Biochemistry and Molecular Biology·P Negri-Cesi, M Motta
Jun 1, 1995·The Journal of Steroid Biochemistry and Molecular Biology·K SundaramC W Bardin
Dec 31, 2003·Bioorganic & Medicinal Chemistry·P P SinghF A Pasha
Jan 10, 1998·Physiology & Behavior·A S ClarkE M Brandling-Bennett
Feb 1, 1987·Baillière's Clinical Endocrinology and Metabolism·U A Knuth, E Nieschlag
Nov 14, 2000·The Journal of Steroid Biochemistry and Molecular Biology·B GonzálezR Manso
Dec 12, 2001·The Journal of Steroid Biochemistry and Molecular Biology·H I Osipova-GoldbergB I Feldkoren
Feb 19, 2003·The Journal of Steroid Biochemistry and Molecular Biology·Andriana D PapaconstantinouKen M Brown
Oct 1, 1996·The Journal of Steroid Biochemistry and Molecular Biology·M D FerrándezR Manso
Aug 14, 2003·Growth Hormone & IGF Research : Official Journal of the Growth Hormone Research Society and the International IGF Research Society·Shalender BhasinThomas W Storer
Feb 16, 2012·Prostate Cancer and Prostatic Diseases·F Azzouni, J Mohler
Dec 20, 2003·The Journals of Gerontology. Series A, Biological Sciences and Medical Sciences·Shalender BhasinNestor F Gonzalez-Cadavid
Oct 27, 2009·Journal of Electron Microscopy·Karina FontanaJohn B Harris
Jan 21, 2003·Biology of Reproduction·Ann S ClarkAndrew C Whitney
Jul 17, 1998·Journal of Acquired Immune Deficiency Syndromes and Human Retrovirology : Official Publication of the International Retrovirology Association·F SattlerR Horton
Aug 1, 1992·Australian and New Zealand Journal of Medicine·M C Kennedy
May 12, 2012·Neuroendocrinology·Joseph G OberlanderLeslie P Henderson
Jul 14, 2004·Sports Medicine·Fred Hartgens, Harm Kuipers
Apr 9, 2014·Current Opinion in Urology·Patrick O Richard, Antonio Finelli
May 13, 1997·Proceedings of the National Academy of Sciences of the United States of America·T M Lin, C Chang
Apr 8, 2014·Bioanalysis·Wadha AbushareedaCostas Georgakopoulos
Jul 1, 1989·Medical Toxicology and Adverse Drug Experience·R C HicksonM T Falduto
May 31, 2013·Disease-a-month : DM·Donald G Barceloux, Robert B Palmer
Dec 31, 2011·The Journal of Steroid Biochemistry and Molecular Biology·Khairat ElBaradieZvi Schwartz
Dec 3, 2011·The Journal of Steroid Biochemistry and Molecular Biology·Laxmi S Inamdar Doddamani, Y Jayamma
Oct 11, 2011·Hormones and Behavior·Ruth I Wood, Steven J Stanton
Feb 16, 2008·Frontiers in Neuroendocrinology·Ruth I Wood
May 27, 2008·British Journal of Pharmacology·A T Kicman

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