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Drug Test Anal ; 13(2): 299-317, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-32852865

RESUMO

ACP-105 is a novel nonsteroidal selective androgen receptor modulator (SARM) with a tissue-specific agonist effect and does not have side effects associated with the use of common androgens. This research reports a comprehensive study for the detection of ACP-105 and its metabolites in racehorses after oral administration (in vivo) and postulating its structures using mass spectrometric techniques. To obtain the metabolic profile of ACP-105, a selective and reliable LC-MS/MS method was developed. The chemical structures of the metabolites were determined based on their fragmentation pattern, accurate mass, and retention time. Under the current experimental condition, a total of 19 metabolites were detected in ACP-105 drug administered equine urine samples. The study results suggest the following: (1) ACP-105 is prone to oxidation, which gives corresponding monohydroxylated, dihydroxylated, and trihydroxylated metabolites; (2) along with oxidation, there is a possibility of elimination of water molecule (dehydration) from the third position of the tropine moiety, resulting in the dehydrated analogs of corresponding monohydroxylated, dihydroxylated, and trihydroxylated metabolites; (3) from the study on the metabolites using LC-MS/MS, it is clear that the fragmentation pattern is identical and a great number of fragment ions are common in all the metabolites and the parent drug. (4) The ACP-105 and its metabolites were detected for up to 72 h; thus, the result is a valuable tool for evaluating its use and/or misuse in sport.


Assuntos
Androgênios/urina , Compostos Azabicíclicos/urina , Cavalos/urina , Espectrometria de Massas em Tandem/métodos , Administração Oral , Androgênios/administração & dosagem , Androgênios/metabolismo , Animais , Compostos Azabicíclicos/administração & dosagem , Compostos Azabicíclicos/metabolismo , Cromatografia Líquida/métodos , Dopagem Esportivo , Feminino , Masculino , Detecção do Abuso de Substâncias/métodos
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