[Synthesis and pharmacologic action of substituted imidazolyl- and thiazolylmethylthioethylguanidine].
Starting with diphenyl N-benzoyl-carbonimidate impromidine analogues characterized by various substituted imidazole or thiazole groups instead of the 5-methylimidazole part have been synthesized and tested for H2-agonistic and H1-antagonistic activity as well. The most potent substances 6h,i are 20-30 times more active than histamine at the H2-receptors in the isolated spontaneously beating guinea-pig right atrium. In isolated perfused guinea-pig hearts 6h,i were found to predominantly stimulate heart rate, whereas the increase in LVdp/dtmax was about 40% of impromidine's maximal response.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D006146:Guanidines / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006439:Hemodynamics / Q000187:drug effects; D006634:Histamine H1 Antagonists / Q000138:chemical synthesis*; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis*; D007082:Ileum / Q000187:drug effects; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects; D009200:Myocardial Contraction / Q000187:drug effects; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D006146:Guanidines; D006634:Histamine H1 Antagonists; D006635:Histamine H2 Antagonists; D007093:Imidazoles; D013844:Thiazoles
Synthese und pharmakologische Wirkung substituierter Imidazolyl- und Thiazolylmethylthioethylguanidine.