Benfenati E, Fanelli R, Bosone E, Caponi R, Farina P
Istituto di Ricerche Farmacologiche Mario Negri, Milan, Italy.
Eur J Drug Metab Pharmacokinet. 1992 Apr-Jun;17(2):93-101. doi: 10.1007/BF03188777.
The compound IBI-P-05006, 2-(6'-carboxyhexyl)-3-n-hexylcyclohexylamine, is an antiaggregating agent under development. IBI-P-05006 is an in vitro inhibitor of platelet aggregation. The biotransformation of this compound has been studied in the dog and rat. We present here a study on the metabolites of IBI-P-05006 found in dog and rat urine, and in dog plasma. Analyses were done by gas chromatography-mass spectrometry. In dog urine 15 metabolites were identified. Some of them were also found in dog plasma and in rat urine. The unmetabolized drug was found only in plasma. 10 different hydroxylated metabolites were characterized. The hydroxyl groups were introduced in the hexyl chain in positions omega-4, omega-3, omega-2, omega-1 and omega.
化合物IBI-P-05006，即2-(6'-羧基己基)-3-正己基环己胺，是一种正在研发的抗聚集剂。IBI-P-05006是血小板聚集的体外抑制剂。该化合物的生物转化已在犬和大鼠中进行了研究。我们在此呈现一项关于在犬尿、大鼠尿以及犬血浆中发现的IBI-P-05006代谢产物的研究。分析通过气相色谱-质谱法进行。在犬尿中鉴定出了15种代谢产物。其中一些也在犬血浆和大鼠尿中被发现。未代谢的药物仅在血浆中被发现。鉴定出了10种不同的羟基化代谢产物。羟基被引入到己基链的ω-4、ω-3、ω-2、ω-1和ω位。
