Heterocyclic環を有するAmidine系化合物の薬理作用(第3報) : 1-Phenyl-4-guanylpiperazine Sulfate(PGP)誘導体の交感神経系に対する作用様式の解明と, Tyramineに対する薬物相互作用

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Pharmacological properties of 1-phenyl-4-guanylpiperazine (PGP) sulfate (I) were examined on various organs innervated by the sympathetic nerve. Effect of PGP derivatives on the acute toxicity of tyramine in mice was also examined with 1-phenyl-(I-PGP), 1-(3-chlorophenyl)-(II), 1-(4-chlorophenyl)-(III), 1-(3-methylphenyl)-(IV), and 1-(4-methylphenyl)-4-guanylpiperazine sulfate (V). The results may be summarized as follows : 1) PGP causes a rise in blood pressure and contraction of the nictitating membrane in spinal cats. These actions are blocked by phentolamine and by pretreatment with reserpine. PGP derivatives potentiate the pressor response induced by tyramine. 2) PGP shows positive inotropic and chronotropic actions on openchest dogs and isolated heart of guinea pigs, but these actions are blocked by DCI and pretreatment with reserpine and guanethidine. 3) PGP causes vasoconstriction on isolated rabbit ear. 4) PGP derivatives increase the acute toxicity of tyramine. There is a correlation between the potentiating action of PGP derivatives on the pressor response of tyramine and their ability to increase the toxicity of tyramine. 5) The sympathomimetic action of PGP might be classified as indirectly acting on the sympathetic nervous system.
公益社団法人日本薬学会の論文
1970-12-25