Heterocyclic環を有するAmidine系化合物の一般薬理作用

抄録

Several heterocyclic amidines, 1-phenyl-(I), 1-(3-chlorophenyl)-(II), 1-(4-chlorophenyl)-(III), 1-(3, 4-dichlorophenyl)-(IV), 1-(3-methylphenyl)-(V), and 1-(4-methylphenyl)-4-guanylpiperazine sulfate (VI), 1-guanylpiperidine sulfate (VII), 1, 4-diguanylpiperazine dihydrochloride (VIII), 4-guanylmorpholine sulfate (IX), and 1-guanylpyrrolidine sulfate (X) were synthesized and examined pharmacologically. 1-Phenyl-4-guanylpiperazine derivatives showed muscle relaxing action and their activities were in the following order : d-tubocurarine>IV, succinylcholine>II, III, V, VI, >I. I, II, III, V, VI, and VII caused a temporary hypotention, while IV, IX, and X showed the pressor action in rats and cats. Pressor action of noradrenaline was not affected and that of tyramine was inhibited by I, II, III, V, and VI. Local anesthetic action, antihistamine, antiacetylcholine, and antiserotonin activities of test compounds were not so strong. Acute toxicities in mice were also tested.