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Metabolic study of a steroid product containing dimethazine using human liver microsomes and a chimeric mouse model

Author
Organization
Abstract
Studies on steroid metabolism are essential to target the best markers for an effective control by anti-doping laboratories. However, ethical objections restrict the use of designer steroids in human administration studies. To overcome these problems alternative in vitro and in vivo models were developed to identify metabolites of new substances and to assure a fast response to evolutions on the steroid market. In this study human liver microsomes and an uPA+/+-SCID chimeric mouse model were used to elucidate the metabolism of a steroid product called ‘Xtreme DMZ’. This product contains the designer steroid dimethazine (DMZ), which consists of two methasterone molecules linked by an azine group. In the performed stability study degradation from dimethazine to methasterone was observed. This degradation was accelerated at a lower pH, with a t1/2 of 23.7 min at 37°C. The high degradation rate at pH 0.5 suggests that an oral administration of dimethazine would lead to a complete degradation of the compound to methasterone in the acidic conditions in the stomach. By a combination of LC-HRMS and GC-MS(/MS) analysis methasterone and six other dimethazine metabolites (M1-M6), which are also methasterone metabolites, could be detected. For an effective control of dimethazine in doping control samples the screening for methasterone and methasterone metabolites should be sufficient. The results of this study will be published elsewhere.
Keywords
metabolism studies, steroids, in-vitro and in-vivo studies, GC-MS/MS, LC-HRMS

Citation

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MLA
Geldof, Lore, Eva Tudela, Leen Lootens, et al. “Metabolic Study of a Steroid Product Containing Dimethazine Using Human Liver Microsomes and a Chimeric Mouse Model.” Recent Advances in Doping Analysis. Ed. Wilhelm Schänzer et al. Vol. 22. Cologne, Germany: Sportverlag Strauss, 2014. 226–226. Print.
APA
Geldof, L., Tudela, E., Lootens, L., Van Lysebeth, J., Meuleman, P., Leroux-Roels, G., Deventer, K., et al. (2014). Metabolic study of a steroid product containing dimethazine using human liver microsomes and a chimeric mouse model. In Wilhelm Schänzer, M. Thevis, H. Geyer, & U. Mareck (Eds.), Recent Advances in Doping Analysis (Vol. 22, pp. 226–226). Presented at the 32nd Cologne workshop of Dope Analysis (Manfred Donike workshop), Cologne, Germany: Sportverlag Strauss.
Chicago author-date
Geldof, Lore, Eva Tudela, Leen Lootens, Jasper Van Lysebeth, Philip Meuleman, Geert Leroux-Roels, Koen Deventer, and Peter Van Eenoo. 2014. “Metabolic Study of a Steroid Product Containing Dimethazine Using Human Liver Microsomes and a Chimeric Mouse Model.” In Recent Advances in Doping Analysis, ed. Wilhelm Schänzer, Mario Thevis, Hans Geyer, and Ute Mareck, 22:226–226. Cologne, Germany: Sportverlag Strauss.
Chicago author-date (all authors)
Geldof, Lore, Eva Tudela, Leen Lootens, Jasper Van Lysebeth, Philip Meuleman, Geert Leroux-Roels, Koen Deventer, and Peter Van Eenoo. 2014. “Metabolic Study of a Steroid Product Containing Dimethazine Using Human Liver Microsomes and a Chimeric Mouse Model.” In Recent Advances in Doping Analysis, ed. Wilhelm Schänzer, Mario Thevis, Hans Geyer, and Ute Mareck, 22:226–226. Cologne, Germany: Sportverlag Strauss.
Vancouver
1.
Geldof L, Tudela E, Lootens L, Van Lysebeth J, Meuleman P, Leroux-Roels G, et al. Metabolic study of a steroid product containing dimethazine using human liver microsomes and a chimeric mouse model. In: Schänzer W, Thevis M, Geyer H, Mareck U, editors. Recent Advances in Doping Analysis. Cologne, Germany: Sportverlag Strauss; 2014. p. 226–226.
IEEE
[1]
L. Geldof et al., “Metabolic study of a steroid product containing dimethazine using human liver microsomes and a chimeric mouse model,” in Recent Advances in Doping Analysis, Cologne, Germany, 2014, vol. 22, pp. 226–226.
@inproceedings{6862114,
  abstract     = {Studies on steroid metabolism are essential to target the best markers for an effective control by anti-doping laboratories. However, ethical objections restrict the use of designer steroids in human administration studies. To overcome these problems alternative in vitro and in vivo models were developed to identify metabolites of new substances and to assure a fast response to evolutions on the steroid market. In this study human liver microsomes and an uPA+/+-SCID chimeric mouse model were used to elucidate the metabolism of a steroid product called ‘Xtreme DMZ’. This product contains the designer steroid dimethazine (DMZ), which consists of two methasterone molecules linked by an azine group. In the performed stability study degradation from dimethazine to methasterone was observed. This degradation was accelerated at a lower pH, with a t1/2 of 23.7 min at 37°C. The high degradation rate at pH 0.5 suggests that an oral administration of dimethazine would lead to a complete degradation of the compound to methasterone in the acidic conditions in the stomach. By a combination of LC-HRMS and GC-MS(/MS) analysis methasterone and six other dimethazine metabolites (M1-M6), which are also methasterone metabolites, could be detected. For an effective control of dimethazine in doping control samples the screening for methasterone and methasterone metabolites should be sufficient. The results of this study will be published elsewhere.},
  author       = {Geldof, Lore and Tudela, Eva and Lootens, Leen and Van Lysebeth, Jasper and Meuleman, Philip and Leroux-Roels, Geert and Deventer, Koen and Van Eenoo, Peter},
  booktitle    = {Recent Advances in Doping Analysis},
  editor       = {Schänzer, Wilhelm and Thevis, Mario and Geyer, Hans and Mareck, Ute},
  isbn         = {9783868840407},
  keywords     = {metabolism studies,steroids,in-vitro and in-vivo studies,GC-MS/MS,LC-HRMS},
  language     = {eng},
  location     = {Cologne, Germany},
  pages        = {226--226},
  publisher    = {Sportverlag Strauss},
  title        = {Metabolic study of a steroid product containing dimethazine using human liver microsomes and a chimeric mouse model},
  volume       = {22},
  year         = {2014},
}