Lampinen-Salomonsson Matilda, Beckman Elin, Bondesson Ulf, Hedeland Mikael
Division of Analytical Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala University, Biomedical Centre, P.O. Box 574, SE-751 23 Uppsala, Sweden.
J Chromatogr B Analyt Technol Biomed Life Sci. 2006 Apr 3;833(2):245-56. doi: 10.1016/j.jchromb.2006.02.014. Epub 2006 Mar 7.
Altrenogest (17alpha-allyl-17beta-hydroxyestra-4,9,11-trien-3-one) is a steroid used for the control of estrus in horses. This drug can potentially be abused in racehorses as the occurrence of estrus can alter their performance. This work describes an analytical method based on liquid chromatography-tandem mass spectrometry for the detection of altrenogest in horse urine down to a concentration of 13 pg/mL (0.042 nM). Furthermore, the qualitative aspect of metabolism of altrenogest in the horse has been studied. The main transformations that were found for this species were conjugation with glucuronic acid and sulfate. These phase II metabolites were identified by molecular mass and by comparison of their collision-induced dissociation product ion spectra with that of the synthetic aglycone at positive and negative potential, respectively. No phase I metabolites were discovered. In order to increase the ionisation in positive electrospray, a derivatisation procedure forming a basic oxime was tested. This process significantly increased the detection sensitivity for altrenogest glucuronide in horse urine.
烯丙孕素（17α-烯丙基-17β-羟基雌甾-4,9,11-三烯-3-酮）是一种用于控制马发情期的甾体药物。由于发情期的出现会影响赛马的表现，这种药物在赛马中可能会被滥用。本文描述了一种基于液相色谱-串联质谱的分析方法，用于检测马尿中低至13 pg/mL（0.042 nM）浓度的烯丙孕素。此外，还研究了烯丙孕素在马体内代谢的定性情况。该物质主要的转化方式是与葡萄糖醛酸和硫酸盐结合。这些II相代谢物通过分子量以及分别在正电位和负电位下将其碰撞诱导解离产物离子光谱与合成苷元的光谱进行比较来鉴定。未发现I相代谢物。为了提高正电喷雾中的离子化程度，测试了一种形成碱性肟的衍生化程序。该过程显著提高了马尿中烯丙孕素葡萄糖醛酸苷的检测灵敏度。
