Borchert H H, Garski P, Pfeifer S
Pharmazie. 1981 Apr;36(4):278-80.
The N-demethylation of various secondary N-methylphenylalkylamines and propylhexedrin in the 9.000-g-supernatant of rat liver homogenates is inhibited by introduction of a N-formyl group. Higher reaction rates for the O-methyl derivatives of pholedrin are attributable to an additional O-demethylation which is obviously favoured, when the N-demethylation is inhibited by the formyl group. The velocity of the oxidative degradation of the methoxymethyl group in formyl(N-methoxymethyl) analogues is markedly higher than the N-demethylation rates of the formyl)N-methyl) derivatives and depends to a greater extent upon the structure of the side-chain and the degree of hydrogenation of the nucleus.
在大鼠肝脏匀浆9000 g上清液中,各种仲N - 甲基苯烷基胺和丙己君的N - 去甲基化受到N - 甲酰基引入的抑制。福来君的O - 甲基衍生物反应速率较高,这归因于额外的O - 去甲基化,当N - 去甲基化被甲酰基抑制时,这种额外的O - 去甲基化显然更有利。甲酰基(N - 甲氧基甲基)类似物中甲氧基甲基的氧化降解速度明显高于甲酰基(N - 甲基)衍生物的N - 去甲基化速率,并且在更大程度上取决于侧链结构和核的氢化程度。