Sports doping: emerging designer and therapeutic β2-agonists

Clin Chim Acta. 2013 Oct 21:425:242-58. doi: 10.1016/j.cca.2013.07.031. Epub 2013 Aug 14.

Abstract

Beta2-adrenergic agonists, or β2-agonists, are considered essential bronchodilator drugs in the treatment of bronchial asthma, both as symptom-relievers and, in combination with inhaled corticosteroids, as disease-controllers. The use of β2-agonists is prohibited in sports by the World Anti-Doping Agency (WADA) due to claimed anabolic effects, and also, is prohibited as growth promoters in cattle fattening in the European Union. This paper reviews the last seven-year (2006-2012) literature concerning the development of novel β2-agonists molecules either by modifying the molecule of known β2-agonists or by introducing moieties producing indole-, adamantyl- or phenyl urea derivatives. New emerging β2-agonists molecules for future therapeutic use are also presented, intending to emphasize their potential use for doping purposes or as growth promoters in the near future.

Keywords: AAF; Beta-agonists; CAS; COMT; COPD; Catechol-O-MethylTransferase; Chronic Obstructive Pulmonary Disease; Court of Arbitration for Sport; Designer drugs; Detection methods; Doping control; ELISA; EU; Enzyme-Linked Immunosorbent Assay; European Union; FDA; Food and Drug Administration; HP-TLC; HRMS; High Performance Thin Layer Chromatography; High Resolution Mass Spectrometry; IAC; ICS; ImmunoAffinity Chromatography; Inhaled Corticosteroid; LABA; LAMA; LC–MS; LOD; Limit of Detection; Liquid Chromatography–Mass Spectrometry; Long-Acting anti-Muscarinic Agent; Long-Acting β(2)-Agonist; MIP; MRPL; Minimum Required Performance Limit; Molecular Imprinted Polymer; MonoAmine Oxidase; PCI; Positive Chemical Ionization; RIA; RadioImmunoAssay; SABA; SPE; SPR; Short-Acting β(2)-Agonist; Solid Phase Extraction; Surface Plasmon Resonance; TLC; TOF; Thin Layer Chromatography; Time-of-Flight; UPLC; UV; Ultra Pressure (or Performance) Liquid Chromatography; Ultraviolet; Veterinary drugs; WADA; World Anti-Doping Agency; adverse analytical finding; ΜΑΟ.

Publication types

  • Review

MeSH terms

  • Adrenergic beta-2 Receptor Agonists / chemical synthesis
  • Adrenergic beta-2 Receptor Agonists / isolation & purification*
  • Adrenergic beta-2 Receptor Agonists / therapeutic use
  • Animals
  • Anti-Inflammatory Agents / chemical synthesis
  • Anti-Inflammatory Agents / isolation & purification*
  • Anti-Inflammatory Agents / therapeutic use
  • Asthma / drug therapy
  • Cattle
  • Designer Drugs / chemical synthesis
  • Designer Drugs / isolation & purification*
  • Dietary Supplements*
  • Doping in Sports / prevention & control*
  • Ethanolamines / chemical synthesis
  • Ethanolamines / isolation & purification
  • Growth Substances / chemical synthesis
  • Growth Substances / isolation & purification
  • Humans
  • Indoles / chemical synthesis
  • Indoles / isolation & purification
  • Quinolones / chemical synthesis
  • Quinolones / isolation & purification
  • Structure-Activity Relationship
  • Sulfonamides / chemical synthesis
  • Sulfonamides / isolation & purification

Substances

  • Adrenergic beta-2 Receptor Agonists
  • Anti-Inflammatory Agents
  • Designer Drugs
  • Ethanolamines
  • Growth Substances
  • Indoles
  • Quinolones
  • Sulfonamides