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布可隆对大鼠哇巴因和地高辛胆汁排泄的增强作用。

Enhancing effect of bucolome on biliary excretion of ouabain and digoxin in the rat.

作者信息

Sato Y, Kanai S, Kitani K

机构信息

First Laboratory of Clinical Physiology, Tokyo Metropolitan Institute of Gerontology, Japan.

出版信息

Res Commun Chem Pathol Pharmacol. 1988 May;60(2):173-89.

PMID:2899336
Abstract

The effect of bucolome (1-cyclohexyl-5-n-butyl-2,4,6-trioxoperhydropyrimidine) on the biliary excretion of intravenously administered ouabain and digoxin was examined in rats. The intravenously administered [3H] ouabain (0.1 mg/100 g b wt) was more rapidly excreted in the bile in female rats than in males. Intraperitoneal administration of bucolome induced a two fold increase in bile flow rate, accompanied by a significant increase in biliary recovery of ouabain during first 10 min (by 100% in males and 50% in females) resulting in significantly higher 60-min total biliary recoveries in both sexes. In female rats 80% of radioactivity was recovered in the bile as an unmetabolized form after 10 min of intravenous administration of [3H] digoxin. Biliary excretion of the parent drug, digoxin, was also enhanced by intraperitoneal administration of bucolome. Although the underlying mechanism(s) remains unknown, it was shown that biliary excretion of both ouabain and digoxin was enhanced by bucolome, as was previously shown for ouabain in male rats.

摘要

在大鼠中研究了布可隆(1-环己基-5-正丁基-2,4,6-三氧代氢化嘧啶)对静脉注射哇巴因和地高辛胆汁排泄的影响。静脉注射的[3H]哇巴因(0.1mg/100g体重)在雌性大鼠胆汁中的排泄速度比雄性大鼠更快。腹腔注射布可隆可使胆汁流速增加两倍,同时在最初10分钟内哇巴因的胆汁回收率显著增加(雄性增加100%,雌性增加50%),导致两性60分钟总胆汁回收率显著提高。在雌性大鼠中,静脉注射[3H]地高辛10分钟后,80%的放射性以未代谢形式在胆汁中回收。腹腔注射布可隆也增强了母体药物地高辛的胆汁排泄。尽管其潜在机制尚不清楚,但研究表明布可隆增强了哇巴因和地高辛的胆汁排泄,这与之前在雄性大鼠中对哇巴因的研究结果一致。

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