Paolini A, D'Incalci M
Cancer Treat Rep. 1986 Apr;70(4):513-6.
The effect of phenobarbital (PB) pretreatment on the N-demethylation and antitumor activity of hexamethylmelamine (HMM) was investigated in mice. In mice pretreated with PB, the levels of HMM in plasma, liver, and M5076 tumor were much lower than in mice treated with HMM alone. Plasma area under the curve (AUC) values were 15 +/- 4 versus 37 +/- 28 micrograms/ml X min, liver AUC values were 43 +/- 13 versus 246 +/- 5 micrograms/g X min, and tumor AUC values were 37 +/- 14 versus 109 +/- 24 micrograms/g X min. All of the N-demethylated metabolites except N2N4 dimethylmelamine in plasma, liver, and tumor also reached much lower levels in mice pretreated with PB. The antitumor activity of HMM was significantly antagonized by PB treatment in both M5076 reticular cell sarcoma and PC6 plasmocytoma of the mouse.
研究了苯巴比妥（PB）预处理对六甲基三聚氰胺（HMM）的N-去甲基化及抗肿瘤活性的影响。在经PB预处理的小鼠中，血浆、肝脏及M5076肿瘤中HMM的水平远低于仅用HMM处理的小鼠。血浆曲线下面积（AUC）值分别为15±4与37±28微克/毫升·分钟，肝脏AUC值分别为43±13与246±5微克/克·分钟，肿瘤AUC值分别为37±14与109±24微克/克·分钟。血浆、肝脏及肿瘤中除N2N4二甲基三聚氰胺外的所有N-去甲基化代谢产物在经PB预处理的小鼠中也达到低得多的水平。在小鼠的M5076网状细胞肉瘤和PC6浆细胞瘤中，PB处理均显著拮抗了HMM的抗肿瘤活性。
