Estus G S, Mieyal J J
Drug Metab Dispos. 1983 Sep-Oct;11(5):471-6.
Deacetylation of a homologous series of alkoxy acetanilides (p-methoxy-, p-ethoxy- (phenacetin), p-(n)-propoxy- and p-(n)-butoxyacetanilide) and three of the corresponding N-hydroxy derivatives was examined in microsomal fractions from the livers and kidneys of C57BL/6J mice. The rates of deacetylation of the phenacetin analogs to the corresponding amines were found to increase with increasing alkyl chain length. With the N-hydroxy derivatives, the apparent KM was found to decrease with increasing chain length, while the Vmax was relatively unaffected. Treatment of the microsomes with the esterase inhibitor bis-p-nitrophenylphosphate resulted in quite similar extents of inhibition of the deacetylation of the phenacetin analogs and their N-hydroxy derivatives.
在C57BL/6J小鼠肝脏和肾脏的微粒体部分中，研究了一系列同系物烷氧基乙酰苯胺（对甲氧基 - 、对乙氧基 - （非那西丁）、对 - （正）丙氧基 - 和对 - （正）丁氧基乙酰苯胺）以及三种相应的N - 羟基衍生物的脱乙酰化情况。发现非那西丁类似物脱乙酰化为相应胺的速率随着烷基链长度的增加而增加。对于N - 羟基衍生物，表观米氏常数（KM）随着链长的增加而降低，而最大反应速率（Vmax）相对不受影响。用酯酶抑制剂双 - 对硝基苯磷酸酯处理微粒体，导致非那西丁类似物及其N - 羟基衍生物脱乙酰化的抑制程度非常相似。
