In vitro histamine H2-antagonist activity of the novel compound HUK 978.
Histamine stimulated adenylate cyclase from guinea-pig fundic mucosa and 3H-tiotidine binding in guinea-pig cerebral cortex were used to assess the in-vitro histamine H2-activity of the novel H2-antagonist HUK 978. The results showed that HUK 978 was a more potent H2-antagonist than either cimetidine or ranitidine. HUK 978 was also shown to be devoid of activity at the histamine H1-receptor, the muscarinic receptor and the alpha and beta-adrenergic receptors.
D000262:Adenylyl Cyclases / Q000378:metabolism; D000818:Animals; D002540:Cerebral Cortex / Q000201:enzymology; D002927:Cimetidine / Q000031:analogs & derivatives / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D005753:Gastric Mucosa / Q000201:enzymology; D006146:Guanidines / Q000494:pharmacology*; D006168:Guinea Pigs; D006632:Histamine / Q000378:metabolism*; D007082:Ileum / Q000201:enzymology; D011968:Receptors, Histamine / Q000378:metabolism*; D011970:Receptors, Histamine H2 / Q000378:metabolism*; D013844:Thiazoles / Q000494:pharmacology*
D006146:Guanidines; D011968:Receptors, Histamine; D011970:Receptors, Histamine H2; D013844:Thiazoles; D002927:Cimetidine; D006632:Histamine; C047021:HUK 978; D000262:Adenylyl Cyclases; C023990:tiotidine