Aminoguanidine系化合物の薬理学的研究(第2報)3,4-Dihydroxy-5-methoxy-benzoylaminoguanidine(AG-2H)の心臓脈管系に対する作用様式の解明

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The pharmacological properties of 3,4-dihydroxy-5-methoxy-benzoylaminoguanidine (AG-2H) on the cardiovascular systems were examined. In the rat and cat, AG-2H (1-5 mg/kg) caused a temporary pressor response which was inhibited by adrenergic α-blocking agents (phentolamine and phenoxybenzamine), but not by hexamethonium and reserpine, while the pressor response was potentiated by cocaine. AG-2H showed a vasoconstriction on the isolated rabbit ear, which was inhibited by phentolamine. The positive inotropic action of the isolated rat and guineapig heart induced by AG-2H (1-3 mg/heart) was slightly inhibited by propranolol. On the other hand, the positive inotropic action of norepinephrine was suppressed by a large dose of AG-2H (5 mg/heart). On the heart of the open chest cat, AG-2H showed an increment of contractile force synchronized with the pressor response. This action was not accompanied by a positive chronotropic action. In the normal and Ca^<2+>-free Krebs-Henseleit solution, AG-2H as well as ouabain slightly prolonged the plateau phase of action potential in the guinea-pig papillary muscle. In the Ca^<2+>-free medium, epinephrine which was effective as other drugs in the normal one, prolonged the plateau phase markedly. From these results, it is suggested that AG-2H posseses mainly a direct sympathomimetic activity on the blood pressure and a musculotropic activity on the heart muscle.
公益社団法人日本薬学会の論文
1972-09-25