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比沙可啶和去乙酰比沙可啶对大鼠体内结肠黏液分泌、黏液合成及电解质转运的影响。

The influence of bisacodyl and deacetylbisacodyl on mucus secretion, mucus synthesis and electrolyte movements in the rat colon in vivo.

作者信息

Farack U M, Gruber E, Loeschke K

出版信息

Eur J Pharmacol. 1985 Nov 5;117(2):215-22. doi: 10.1016/0014-2999(85)90606-5.

Abstract

The effect of the diphenolic laxatives bisacodyl and deacetylbisacodyl on mucus secretion and fluid, sodium and potassium net transport was studied in rat colon perfused in vivo. Mucus output in the effluent was determined as total protein-bound hexose. Deacetylbisacodyl was more potent than the parent compound and was used to investigate dose-response relationships. At a low concentration (0.1 mg/dl), mucus and potassium secretion were stimulated whereas sodium and fluid absorption were inhibited, or converted to secretion, only at higher concentrations (0.5-3.0 mg/dl). All effects were dose-dependent and reversible within 1 h. With longer lasting perfusion of deacetylbisacodyl, mucus appeared in two peaks, one initial peak and another after 4 h. The late peak contained newly synthetized glycoproteins as indicated by the incorporation of intravenously injected [14C]galactose. It is concluded that stimulation of mucus secretion and synthesis contributes to the laxative action of bisacodyl. The effects of low versus high concentrations suggests that part of the potassium secretion is due to mucus release.

摘要

在体内灌注的大鼠结肠中,研究了双酚类泻药比沙可啶和去乙酰比沙可啶对黏液分泌以及液体、钠和钾净转运的影响。流出物中的黏液输出量通过总蛋白结合己糖来测定。去乙酰比沙可啶比母体化合物更有效,被用于研究剂量反应关系。在低浓度(0.1毫克/分升)时,黏液和钾的分泌受到刺激,而钠和液体的吸收受到抑制,或者只有在较高浓度(0.5 - 3.0毫克/分升)时才转变为分泌。所有效应均呈剂量依赖性,且在1小时内可逆。随着去乙酰比沙可啶灌注时间延长,黏液出现两个峰值,一个是初始峰值,另一个在4小时后出现。如静脉注射[14C]半乳糖的掺入所示,后期峰值包含新合成的糖蛋白。得出的结论是,黏液分泌和合成的刺激有助于比沙可啶的泻药作用。低浓度与高浓度的效应表明,部分钾分泌是由于黏液释放所致。

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