Valerino D M, Vesell E S, Stevens J T, Rudnick S L
Pharmacology. 1978;17(2):113-7. doi: 10.1159/000136843.
When administered by intraperitoneal injection daily for 3, 7 or 14 days, pargyline (75 mg/kg) significantly reduced rat hepatic microsomal ethylmorphine N-demethylase activity and cytochrome P-450 content. Injection of a lower dose of pargyline (15 mg/kg) failed to alter significantly either ethylmorphine N-demethylase activity or cytochrome P-450 content. Studies performed in vitro reveal that pargyline is metabolized to at least three compounds by rat hepatic microsomes. Thin-layer chromatography and other analyses suggest that one metabolite is an N-demethylated form, norpargyline.
每天腹腔注射3、7或14天，优降宁（75毫克/千克）可显著降低大鼠肝微粒体N-脱甲基酶活性及细胞色素P-450含量。注射较低剂量的优降宁（15毫克/千克）则不会显著改变N-脱甲基酶活性或细胞色素P-450含量。体外研究表明，优降宁可被大鼠肝微粒体代谢为至少三种化合物。薄层色谱法和其他分析表明，其中一种代谢产物是N-去甲基化形式，即去甲优降宁。
