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:采用人肝微粒体在体外研究尼莫地平 (Nim)在人体内的代谢物及代谢途径 . Nim在人肝微粒体内被迅速代谢成 3个代谢物 ,分别是 Nim二氢吡啶环脱氢代谢物 M1,二氢吡啶环侧链脱甲基代谢物M2 ,二氢吡啶环脱氢及其侧链脱甲基代谢物 M3.Nim在人肝微粒体中的最初的两步代谢反应是其二氢吡啶环脱氢氧化及其侧链脱甲基反应 ,两者的代谢产物可以被进一步代谢为代谢物 M3.CYP3A的特异性抑制剂醋竹桃霉素和酮康唑可以抑制Nim的二氢吡啶环脱氢氧化及其侧链脱甲基反应 ,使 Nim的代谢速率明显下降 ,结果提示 CYP3A参与了 Nim在人肝微粒体内的代谢
: In vitro studies of the metabolites and metabolic pathways of Nim in humans using human liver microsomes. Nim is rapidly metabolized in human liver microsomes to three metabolites, Nim dihydropyridine ring, M1, the dihydropyridine ring side chain demethylation metabolite M2, the dihydropyridine ring dehydrogenation and its side chain demethylation metabolite M3.Nim’s initial two-step metabolic response in human liver microsomes is its two Hydrogen pyridine ring dehydrogenation and its side chain demethylation reaction, the two metabolites can be further metabolized to metabolites M3.CYP3A specific inhibitors vine oleandomycin and ketoconazole can inhibit the Nim dihydrogen The dehydrogenation of pyridine ring and the demethylation of its side chain led to a significant decrease in the rate of Nim metabolism, suggesting that CYP3A is involved in the metabolism of Nim in human liver microsomes