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氯丙嗪在大鼠胃肠道中的分布及其对吸收功能的影响。

Distribution of chlorpromazine in the gastrointestinal tract of the rat and its effect on absorptive function.

作者信息

Sundaresan P R, Rivera-Calimlim L

出版信息

J Pharmacol Exp Ther. 1975 Sep;194(3):593-602.

PMID:240020
Abstract

The distribution of [14C]chlorpromazine was studied in segments of the gastrointestinal tract of the rat after an oral dose of 20 mg/kg (1-2 muc). The total radioactivity in the gastrointestinal tract was, respectively, 43.2 +/- 3.6, 28.9 +/- 2.2 and 14.1 +/- 1.1 (mean +/- S.E. percent administered dose) at 2, 6 and 24 hours after dosing. The maximum observed total radioactivity in the different segments occurred at different times after dosing. The percentage of total radioactivity present in each tissue as unchanged [14C]chlorpromazine decreased with time in all the tissues. At all time points, this parameter also showed a consistent pattern: % stomach greater than % duodenum greater than % jejunum greater than % ileum. The effect of chronic administration of [14C]chlorpromazine on intestinal absorptive function was studied by the everted sac technique. Mucosal transport of L-[14C]methionine was significantly inhibited (24.4% of control), but no effect on transport of D-[14C]xylose was observed.

摘要

在大鼠口服20mg/kg(1-2μc)剂量的[14C]氯丙嗪后,研究了其在大鼠胃肠道各段的分布情况。给药后2、6和24小时,胃肠道中的总放射性分别为43.2±3.6、28.9±2.2和14.1±1.1(平均值±标准误,占给药剂量的百分比)。不同肠段观察到的最大总放射性出现在给药后的不同时间。各组织中以未变化的[14C]氯丙嗪形式存在的总放射性百分比随时间在所有组织中均下降。在所有时间点,该参数也呈现出一致的模式:胃的百分比>十二指肠的百分比>空肠的百分比>回肠的百分比。通过外翻肠囊技术研究了长期给予[14C]氯丙嗪对肠道吸收功能的影响。L-[14C]蛋氨酸的黏膜转运受到显著抑制(为对照的24.4%),但未观察到对D-[14C]木糖转运的影响。

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