BOSENTAN ANTAGONIZES THE EFFECTS OF ENDOTHELIN-1 ON RAT GASTRIC BLOOD-FLOW AND MUCOSAL INTEGRITY

被引：14

作者：

LAZARATOS, S

NAKAHARA, A

GOTO, K

FUKUTOMI, H

机构：

[1] UNIV TSUKUBA, INST CLIN MED, DEPT INTERNAL MED, TSUKUBA, IBARAKI 305, JAPAN

[2] UNIV TSUKUBA, DEPT PHARMACOL, TSUKUBA, IBARAKI 305, JAPAN

来源：

LIFE SCIENCES | 1995年 / 56卷 / 09期

关键词：

ENDOTHELIN-1; BOSENTAN; GASTRIC ULCER; GASTRIC MUCOSAL BLOOD FLOW;

D O I：

10.1016/0024-3205(94)00506-N

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 [基础医学];

摘要：

Bosentan, a new type of orally effective, mixed (ETA+ETB) endothelin receptor antagonist has been recently introduced and tested in a variety of experimental models. We studied the effect of bosentan on the changes in gastric mucosal hemodynamics and mucosal integrity, induced by the exogenous application of endothelin-1, in rats. Bosentan (10 mg/kg iv) pretreated rats were injected with endothelin-1 (500-1000-2000 pmol/kg, iv) and gastric mucosal hemodynamics were monitored. After combined oral (30 mg/kg) and systemic pretreatment with bosentan we studied the effects of submucosal injection of endothelin-1 (50 pmol) on blood flow and gastric mucosa. Bosentan antagonized the vasodilator, vasoconstrictor and ulcerogenic effects of endothelin-1 in the rat gastric mucosa. These results show that bosentan can be a useful probe in the study of endogenous endothelin in the gastrointestinal tract.

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收藏

页码：PL195 / PL200

页数：6

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