Oruç E E, Kabasakal L, Rollas S
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, Istanbul, Turkey.
Eur J Drug Metab Pharmacokinet. 2003 Apr-Jun;28(2):113-8. doi: 10.1007/BF03190498.
The purpose of this study was to investigate the in vivo metabolism of 5-(4-nitrophenyl)-4-(2-phenylethyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione. First its potential metabolites were synthesized and then the structures of the original compound were elucidated by UV, 1H-NMR and elemantary analysis. 40 mg dose was given intraperitoneally to rats. Blood samples were collected at 0, 0.5, 1, 2, 4, 6, 12, 24, 48 and 72 hours after administration of substrate and blood was centrifuged to obtain plasma. The plasma were passed through a Sep-Pak C18 cartridge. The samples were separated using HPLC on a reverse phase system. This study revealed reduction, N-acetylation and N-dealkylation as pathway of 5-(4-nitrophenyl)-4-(2-phenylethyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione metabolism.
本研究的目的是研究5-(4-硝基苯基)-4-(2-苯乙基)-2,4-二氢-3H-1,2,4-三唑-3-硫酮的体内代谢情况。首先合成其潜在代谢产物,然后通过紫外光谱、¹H-核磁共振和元素分析对原始化合物的结构进行了阐明。给大鼠腹腔注射40毫克剂量。在给予底物后的0、0.5、1、2、4、6、12、24、48和72小时采集血样,将血液离心以获得血浆。血浆通过Sep-Pak C18柱。样品在反相系统上用高效液相色谱法进行分离。本研究揭示了还原、N-乙酰化和N-脱烷基化是5-(4-硝基苯基)-4-(2-苯乙基)-2,4-二氢-3H-1,2,4-三唑-3-硫酮的代谢途径。