[Synthesis and pharmacologic action of arylmethylethylguanidines].
Impromidine analogous guanidines have been prepared characterized by H2-unspecific arylmethyl groups instead of the 5-methylimidazole residue. The most potent substances proved to be about 20 times more active than histamine at the isolated spontaneously beating guinea-pig right atrium (H2-agonism), simultaneously showing moderate H1-antagonistic activity at the guinea-pig ileum. In isolated perfused guinea-pig hearts the thenylthioethylguanidine 9e was very potent in increasing LVdp/dtmax, achieving about 90% of impromidine's maximal response. In comparison with impromidine the increase in heart rate was lower and rhythm disturbances were substantially reduced.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D006146:Guanidines / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D006439:Hemodynamics / Q000187:drug effects; D006634:Histamine H1 Antagonists / Q000138:chemical synthesis*; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D009130:Muscle, Smooth / Q000187:drug effects
D006146:Guanidines; D006634:Histamine H1 Antagonists
Synthese und pharmakologische Wirkung von Arylmethylthioethylguanidinen.