open access
Duality nature of Selective Androgen Receptor Modulators and Specific Steroids Substance
, 2
Affiliations- Lazarski University, Warsaw, Poland
- The Polish Anti-Doping Laboratory, Warsaw, Poland
open access
Abstract
Selective Androgen Receptor Modulators (SARMs) are the novel class of the androgen receptors (AR), often called tissue-selective AR ligands. Discovery of SARMs will give a possibility to the alternative therapy for androgens therapy (osteoporosis, prostate cancer, muscle wasting). SARMs should have high specificity for the AR, tissue-selective pharmacokinetic activities, improved oral bioavailability and pharmacokinetic profile which allows once-a-day administration [1].
Example of SARMs is flutamide (flutamidum, Eulexin, imid 2-methyl-N-{4-nitro-(3-trifluoromethyl)-phenyl]- propionic acid), a synthetic nonsteroidal drug that is a competitive antagonist of the androgen receptor. SARMs were recognized as forbidden substances by the World Anti-Doping Agency (WADA) and since 2004 they are on the Prohibited List. To point on the Prohibited List 2019 “Substance and methods prohibited at all time (in- and out-of-competition)” SARMs belong to group S1. 2. Other Anabolic Agents, and to group S4. Hormone Antagonist and Modulators [2].
The main role of an anti-doping laboratory is to analyse and to determine whether a given substance should be prohibited in sport. The principal analyses of SARMs and Specific Steroid Substance are a different variant of chromatography (LC — liquid or GC — gas) with many detection techniques (MS — mainly mass spectrometer, MS/MS — tandem mass spectrometer).
Abstract
Selective Androgen Receptor Modulators (SARMs) are the novel class of the androgen receptors (AR), often called tissue-selective AR ligands. Discovery of SARMs will give a possibility to the alternative therapy for androgens therapy (osteoporosis, prostate cancer, muscle wasting). SARMs should have high specificity for the AR, tissue-selective pharmacokinetic activities, improved oral bioavailability and pharmacokinetic profile which allows once-a-day administration [1].
Example of SARMs is flutamide (flutamidum, Eulexin, imid 2-methyl-N-{4-nitro-(3-trifluoromethyl)-phenyl]- propionic acid), a synthetic nonsteroidal drug that is a competitive antagonist of the androgen receptor. SARMs were recognized as forbidden substances by the World Anti-Doping Agency (WADA) and since 2004 they are on the Prohibited List. To point on the Prohibited List 2019 “Substance and methods prohibited at all time (in- and out-of-competition)” SARMs belong to group S1. 2. Other Anabolic Agents, and to group S4. Hormone Antagonist and Modulators [2].
The main role of an anti-doping laboratory is to analyse and to determine whether a given substance should be prohibited in sport. The principal analyses of SARMs and Specific Steroid Substance are a different variant of chromatography (LC — liquid or GC — gas) with many detection techniques (MS — mainly mass spectrometer, MS/MS — tandem mass spectrometer).
Keywords
SARMs; SERMs; antiandrogens; antiestrogens; doping analysis
About this articleTitle
Duality nature of Selective Androgen Receptor Modulators and Specific Steroids Substance
Journal
Disaster and Emergency Medicine Journal
Issue
Article type
Review paper
Pages
60-62
Published online
2019-08-06
Page views
1099
Article views/downloads
778
DOI
Bibliographic record
Disaster Emerg Med J 2019;4(2):60-62.
Keywords
SARMs
SERMs
antiandrogens
antiestrogens
doping analysis
Authors
Damian Gorczyca
Dorota Kwiatkowska
References (6)- Wenqing G, Dalton JT. Drug Discovery Today. 2007; 12: 241.
- World Anti-Doping Agency: The 2019 prohibited list, World Anti-Doping Agency, Montreal (2019). http://www.wada-ama.org/rtecontent/document/2019_List_En.pdf (14.07.2019).
- Macgregor JI, Jordana C. Pharmacological Reviews. 1998; 50: 151.
- Gjerde J, et al. Chromatogr A. 2005; 1082: 6.
- Thevis M., Kamber M., Schänzer W. Proceeding of the 5th Workshop on Dope analysis. Cologne, 2000.
- World Anti-Doping Agency: WADA annually publishes statistical reports as reported by the WADA-accredited laboratories in ADAMS, 2017 Anti-Doping Testing Figures Report - Executive Summary (online 14.07.2019).