Aminoguanidine系化合物の薬理学的研究(第1報) : Aryloylaminoguanidine並びにその関連Triazole化合物の一般薬理作用

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Aminoguanidines and triazoles were synthesized and their general pharmacological actions were examined. Test compounds were benzoyl-(I), 3-hydroxy-4,5-dimethoxybenzoyl-(II), 3-benzyloxy-4,5-dimethoxybenzoyl-(III), 3,4,5-trimethoxybenzoyl-(IV), nicotinoyl-(V), isonicotinoyl-(VI), 3,4-dihydroxy-5-methoxybenzoyl aminoguanidines (X) and 3-phenyl-(VII), 3-(3'-pyridyl)-(VIII), and 3-(4'-pyridyl)-5-amino-1,2,4-triazoles (IX). Among these compounds, II, III, and X showed interesting pharmacological actions. II produced a contractile response in the small intestine of a mouse, which was inhibited by procaine and atropine but not by hexamethonium or morphine, while the response was potentiated by a cholinesterase inhibitor. Therefore, II possesses a muscarinic property. However, the nicotinic action did not appear. III showed a papaverine-like action ; contraction of the small intestine evoked by ACh and BaCl_2 was surpressed by III. III showed the anti-Ba^<2+> action half as potent as papaverine. On the rat blood pressure, X had a potent presser action which was blocked by phentolamine. Also, a positive inotropic action appeared on the isolated rat heart. With the exception of X, a correlation of the pharmacological activity with acute toxicity of the test compounds was observed in this experiment.
公益社団法人日本薬学会の論文
1972-04-25