EFFECTS OF IMIDAZOLINES AND DERIVATIVES ON INSULIN-SECRETION AND VASCULAR-RESISTANCE IN PERFUSED RAT PANCREAS

被引:34
作者
BERDEU, D
GROSS, R
RIBES, G
LOUBATIERESMARIANI, MM
BERTRAND, G
机构
[1] FAC MED MONTPELLIER,INST BIOL,PHARMACOL LAB,F-34060 MONTPELLIER,FRANCE
[2] CNRS,INSERM,CTR PHARMACOL ENDOCRINOL,UPR 9023,F-34094 MONTPELLIER,FRANCE
关键词
IMIDAZOLINE; OXAZOLINE; IMIDAZOLINE SITE; INSULIN SECRETION; VESSEL; PANCREAS; RAT;
D O I
10.1016/0014-2999(94)90378-6
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The effects of imidazolines and derivatives were studied on insulin secretion and vascular resistance in the isolated perfused rat pancreas. On insulin secretion, two imidazoline alpha(2)-adrenoceptor antagonists, efaroxan (1-100 mu M) and RX821002 (10 mu M), had a stimulating response; however, idazoxan, like the non-imidazoline alpha(2)-adrenoceptor antagonist yohimbine, was ineffective at 10 mu M. The oxazoline rilmenidine with alpha(2)-adrenergic activity at 10 mu M inhibited insulin release; this effect was reversed to a stimulation after the blockade of alpha(2)-adrenoceptors. Antazoline (1-10 mu M), an imidazoline devoid of alpha(2)-adrenergic activity, also had an insulin-releasing effect. On pancreatic vessels, all imidazolines tested (efaroxan, RX821002, antazoline and idazoxan), in contrast to yohimbine, induced vasoconstriction. Rilmenidine did not have a vasoconstrictor effect after blockade of alpha(2)-adrenoceptors. Furthermore, the efaroxan-induced insulin release or vasoconstriction was not affected by the blockade of alpha(2)- and alpha(1)-adrenoceptors. This study shows that imidazolines and derivatives are able to stimulate insulin release and induce vasoconstriction in the rat pancreas. These effects cannot be ascribed to an interaction with alpha-adrenoceptors but may involve different types of imidazoline sites.
引用
收藏
页码:119 / 125
页数:7
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