Structural characteristics of anabolic androgenic steroids contributing to binding to the androgen receptor and to their anabolic and androgenic activities Applied modifications in the steroidal structure

  title={Structural characteristics of anabolic androgenic steroids contributing to binding to the androgen receptor and to their anabolic and androgenic activities Applied modifications in the steroidal structure},
  author={Argyro G Fragkaki and Yiannis S Angelis and Michael A. Koupparis and Anna Tsantili-Kakoulidou and George Kokotos and Constantinos D. Georgakopoulos},

Anabolic Androgenic Steroid (AAS) Related Deaths: Autoptic, Histopathological and Toxicological Findings

The aim of this review is to focus on deaths related to AAS abuse, trying to evaluate the autoptic, histopathological and toxicological findings in order to investigate the pathophysiological mechanism that underlines this type of death, which is still obscure in several aspects.

[Myoanabolic steroids and selective androgen receptor modulators: mechanism of action and perspectives].

  • M. Tóth
  • Biology, Medicine
    Orvosi hetilap
  • 2009
An explanation put forward by us in 1982 for the mechanism of the preferential myotropic effect of nandrolone (19-nortestosterone) exploits the fundamental difference between the 5alpha-reductase concentrations in skeletal muscle and androgenic target tissue.

The Buzz about Anabolic Androgenic Steroids: Electrophysiological Effects in Excitable Tissues

The known effects of AAS on molecular targets that play critical roles in controlling electrical activity are reviewed, with a specific focus on the effects of Anabolic androgenic steroids on neurotransmission mediated by GABAA receptors in the central nervous system.

Anabolic-androgenic steroids and cardiovascular risk

The use/abuse of AAS is correlated with higher cardiovascular risks, and many AAS users/abusers had cardiovascular diseases, however, there are many confounding factors in the studies that explored the causality between AAS intake and disease development, and additional studies are required to determine AAS toxicity.

Anabolic Androgenic Steroid Abuse: Multiple Mechanisms of Regulation of GABAergic Synapses in Neuroendocrine Control Regions of the Rodent Forebrain

How exposure to AAS alters GABAergic transmission and neural activity within these forebrain regions is reviewed, taking advantage of in vitro systems and both wild‐type and genetically altered mouse strains to better understand how these synthetic steroids affect the neural systems that underlie the regulation of reproduction and the expression of sexual behaviours.

In Vitro Synthesis of Metabolites of three Anabolic Androgenic Steroids, by Human Liver Microsomes

The aim of this thesis was to synthesize and identify metabolites from known and rare anabolic androgenic steroids, by the use of human liverMicrosomes, by incubating AAS with human liver microsomes and co factors.

Synthesis of sex hormone-derived modified steroids possessing antiproliferative activity

Characterization of identity, metabolism and androgenic activity of 17-hydroxyandrosta-3,5-diene by GC–MS and a yeast transactivation system

Giving attention to the androgenic potential of steroidal dietary supplements, the analysis using both mass spectrometry techniques and the YAS-based assay on the product “Syntrax Tetrabol” which was a confiscated dietary supplement and marketed as a steroid precursor was exemplified.

Anabolic Steroid use in Sports and in Physical Activity: Overview and Analysis

AAS were the first identifying doping agents that have ergogenic eff ects and are on the International Olympic Committee’s list of banned substances and represent only one of many classes of agents it is important to used by recreational bodybuilders and by athletes in the 21st century.



Steroid structure and androgenic activity. Specificities involved in the receptor binding and nuclear retention of various androgens.

It is found that many potent synthetic androgens can bind directly to β protein and to prostate cell nuclei without a metabolic conversion, indicating that the bulkiness and flatness of the steroid molecule play a more important role in receptor binding than the detailed electronic structure at the Δ4 bond of Ring A.

Different patterns of metabolism determine the relative anabolic activity of 19-norandrogens

Metabolism of Anabolic-Androgenic Steroids

Anabolic-Androgenic Steroids (AAS) Structure, Nomenclature, Classification, and AAS Biological Properties, Role of AAS in Metabolism Regulation in Norm and Pathology and use in Medicine and Cattle Breeding.

Pharmacokinetics and Pharmacodynamics of Nonsteroidal Androgen Receptor Ligands

This review focuses on the pharmacokinetics, metabolism, and pharmacology of clinically used and emerging nonsteroidal AR ligands, including antagonists, agonists, and selective androgen receptor modulators.

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.

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.

Biological function and mode of action of the androgen receptor

Environmental androgens can be precursors of the naturally occurring biologically active androgens testosterone and dihydrotestosterone or result from anabolic steroid use in the livestock industry, and have agonist activity by their ability to bind the AR and mimic the natural hormone, increasing AR-mediated transcription of androgen-responsive genes.

Nonsteroidal selective androgen receptors modulators (SARMs): designer androgens with flexible structures provide clinical promise.

  • T. Brown
  • Biology, Medicine
  • 2004
Nonsteroidal androgen ligands demonstrate tissue-selective actions and diverse activity profiles that serve specific therapeutic needs and are referred to as pure antiandrogens because they bind exclusively to AR and thus are devoid of antigonadotropic, antiestrogenic, and progestational effects.