Rivera-Calimlim L
Br J Pharmacol. 1974 Feb;50(2):259-63. doi: 10.1111/j.1476-5381.1974.tb08570.x.
1 The absorption, tissue distribution, and metabolism of [(14)C]-O-methyldopa were compared with those of [(14)C]-L-DOPA after oral administration to rats.2 Total radioactivity in the plasma and brain of rats treated with [(14)C]-O-methyldopa was significantly higher (2 fold and 30-50 fold, respectively) than that of rats treated with [(14)C]-L-DOPA.3 Total radioactivity in the gut washings and intestinal tissue 2 h after oral administration was significantly higher in rats treated with [(14)C]-L-DOPA than in rats treated with [(14)C]-O-methyldopa. The reverse was observed in the stomach tissues.4 Peripheral metabolism of [(14)C]-O-methyldopa was much lower than that of [(14)C]-L-DOPA; the major metabolite of [(14)C]-O-methyldopa in the plasma is L-DOPA, whereas L-DOPA is mainly metabolized to phenylcarboxylic acids.
将[(14)C]-O-甲基多巴和[(14)C]-L-多巴口服给予大鼠后,比较它们的吸收、组织分布和代谢情况。
用[(14)C]-O-甲基多巴处理的大鼠血浆和脑中的总放射性明显高于用[(14)C]-L-多巴处理的大鼠(分别高2倍和30 - 50倍)。
口服给药2小时后,用[(14)C]-L-多巴处理的大鼠肠冲洗液和肠组织中的总放射性明显高于用[(14)C]-O-甲基多巴处理的大鼠。在胃组织中观察到相反的情况。
[(14)C]-O-甲基多巴的外周代谢远低于[(14)C]-L-多巴;[(14)C]-O-甲基多巴在血浆中的主要代谢产物是L-多巴,而L-多巴主要代谢为苯羧酸。