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大鼠口服(14C)-O-甲基多巴和(14C)-L-多巴后的吸收、代谢及分布

Absorption, metabolism and distribution of (14C)-O-methyldopa and (14C)-L-dopa after oral administration to rats.

作者信息

Rivera-Calimlim L

出版信息

Br J Pharmacol. 1974 Feb;50(2):259-63. doi: 10.1111/j.1476-5381.1974.tb08570.x.

Abstract

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.

摘要
  1. 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。

  2. 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)。

  3. 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。

  4. [(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。

相似文献

4
The metabolism of L-3-O-methyldopa, a precursor of dopa in man.
Clin Pharmacol Ther. 1971 Jul-Aug;12(4):678-82. doi: 10.1002/cpt1971124678.

本文引用的文献

1
The metabolism of L-3-O-methyldopa, a precursor of dopa in man.
Clin Pharmacol Ther. 1971 Jul-Aug;12(4):678-82. doi: 10.1002/cpt1971124678.
2
Absorption and metabolism of L-dopa by the human stomach.左旋多巴在人体胃部的吸收与代谢
Eur J Clin Invest. 1971 May;1(5):313-20. doi: 10.1111/j.1365-2362.1971.tb00637.x.
4
Distribution and metabolism of L-3-O-methyldopa in rats.L-3-O-甲基多巴在大鼠体内的分布与代谢
Br J Pharmacol. 1970 Nov;40(3):461-7. doi: 10.1111/j.1476-5381.1970.tb10627.x.
6
L-3,4-dihydroxyphenylalanine metabolism by the gut in vitro.
Biochem Pharmacol. 1971 Nov;20(11):3051-7. doi: 10.1016/0006-2952(71)90109-2.
9
Parkinsonism treated with 3-O-methyldopa.
Clin Pharmacol Ther. 1973 May-Jun;14(3):386-9. doi: 10.1002/cpt1973143386.

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