LC-MS^n鉴定2-羟基-1-甲氧基阿朴啡在Beagle犬体内的主要代谢产物

Identification of Major Metabolites of 2-Hydroxy-1-Methoxyaporphine in Beagle Dogs Plasma by Liquid Chromatography/Ion Trap Mass Spectrometry

目的研究2-羟基-1-甲氧基阿朴啡在Beagle犬体内的代谢行为。方法选择健康Beagle犬3只单剂量1.5×10-3g·kg-1灌胃2-羟基-1-甲氧基阿朴啡,于给药后60min前肢静脉取血,3000r·min-1离心10min,分取血浆,将血浆经SPE-C18固相柱纯化后,采用LC-MSn方法对血浆中待测代谢产物进行总离子监测(TIM)和多级全扫描质谱分析(MSn)。结果在Beagle犬血浆中检测到母体成分2-羟基-1-甲氧基阿朴啡和3种代谢产物。结论2-羟基-1-甲氧基阿朴啡在Beagle犬体内主要与葡萄糖醛酸相结合形成II相代谢产物。

OBJECTIVE To investigate the major metabolites of 2-hydroxy-1-methoxyaporphine in Beagle dogs. METHODS The blood samples were collected from vein after a single dose of 1.5 mg.kg-1 2-hydroxy-1-methoxyaporphine. The plasma samples were purified by a SPE column （SPE-CIs） and analyzed with LC/MSn for potential metabolites. RESULTS 2-hydroxy-l-methoxyaporphine and its three metabolites were first identified in Beagle dogs plasma. CONCLUSION The major metabolic pathway of 2-hydroxy-1-methoxyaporphine in Beagle dogs is conjugating with glucuronic acid, forming phase II mctabolites.