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曲培卡因及其某些衍生物对应激大鼠胃壁黏液的影响。

Effect of trapencaine and some of its derivatives on gastric wall mucus in stressed rats.

作者信息

Nosálová V, Juránek I, Babulová A

机构信息

Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava.

出版信息

Pharmazie. 1995 Jun;50(6):424-5.

PMID:7651982
Abstract

The effect of selected carbanilates on the rat gastric mucus was tested after oral administration. The compounds K 1905 and K 2002 were found to increase gastric mucus content in nonstressed rats while compound P 2 was ineffective. The activity of K 1905 was comparable with that of the parent drug trapencaine. Cold-restraint stress decreased the gastric mucus content and induced haemorrhagic erosions in the glandular stomach. With the exception of compound P 2 pretreatment with carbanilates dose-dependently diminished the extent of stress-induced gastric damage and prevented the depletion of mucus after stress. The results indicate that pentyloxy-substitution in the meta and in the para position on the benzene ring of the parent structure (K 1905 and K 2002, respectively) seems to be more suitable for mucus enhancing activity than alkyloxy-substitution on the para position (P 2). The observed increased mucus secretion might be partly responsible for the gastroprotective action of the drugs tested.

摘要

经口服给药后,测试了所选氨基甲酸酯类化合物对大鼠胃黏液的影响。发现化合物K 1905和K 2002可增加非应激大鼠的胃黏液含量,而化合物P 2则无效。K 1905的活性与母体药物曲喷卡因相当。冷束缚应激会降低胃黏液含量,并在腺胃中诱发出血性糜烂。除化合物P 2外,氨基甲酸酯类化合物预处理可剂量依赖性地减轻应激诱导的胃损伤程度,并防止应激后黏液耗竭。结果表明,母体结构苯环间位和对位的戊氧基取代(分别为K 1905和K 2002)似乎比对位的烷氧基取代(P 2)更适合增强黏液活性。观察到的黏液分泌增加可能部分归因于所测试药物的胃保护作用。

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