The influence of guanidino and isothiourea groups in histaminergic compounds on H2-activity.
Because in some alkylenediisothioureas replacement of one of the isothiourea groups by a guanidino group resulted in a strong increase in agonistic histamine H2-activity, while replacement of the guanidino group of a potent analogue of impromidine by an isothiourea group resulted in a complete loss of histamine H2-activity, it was concluded that guanidino and isothiourea groups are not bio-isosteric for the H2-receptor.
D000818:Animals; D006168:Guinea Pigs; D007093:Imidazoles / Q000494:pharmacology*; D017446:Impromidine; D066298:In Vitro Techniques; D011968:Receptors, Histamine / Q000187:drug effects*; D011970:Receptors, Histamine H2 / Q000187:drug effects*; D013329:Structure-Activity Relationship
D007093:Imidazoles; D011968:Receptors, Histamine; D011970:Receptors, Histamine H2; D017446:Impromidine