Specific activation of cyclic AMP-dependent protein kinase(s) by H2-histamine agonists in isolated gastric mucosal cells from guinea-pig.
Histamine stimulated cyclic AMP-dependent protein kinase activity in dispersed mucosal cells from guinea-pig gastric fundus (Ka = 5 microM). The H2-agonists dimaprit and impromidine produced similar effects, while the H1-agonist 2-(2-pyridyl) ethylamine had only a weak one. The H2-antagonist cimetidine competitively inhibited 0.1 mM histamine stimulation (Ki = 2 microM). In contrast, the H1-antagonist diphenhydramine had no effect up to 1 mM.
D000818:Animals; D002927:Cimetidine / Q000494:pharmacology; D000242:Cyclic AMP / Q000494:pharmacology*; D017259:Dimaprit; D004155:Diphenhydramine / Q000494:pharmacology; D004789:Enzyme Activation / Q000187:drug effects; D005753:Gastric Mucosa / Q000187:drug effects* / Q000378:metabolism; D006146:Guanidines / Q000494:pharmacology*; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D007093:Imidazoles / Q000494:pharmacology*; D017446:Impromidine; D066298:In Vitro Techniques; D011494:Protein Kinases / Q000378:metabolism*; D011725:Pyridines / Q000494:pharmacology*; D011968:Receptors, Histamine / Q000187:drug effects*; D011970:Receptors, Histamine H2 / Q000187:drug effects*; D013890:Thiourea / Q000494:pharmacology*
D006146:Guanidines; D007093:Imidazoles; D011725:Pyridines; D011968:Receptors, Histamine; D011970:Receptors, Histamine H2; D002927:Cimetidine; D006632:Histamine; D004155:Diphenhydramine; D017446:Impromidine; C006183:2-(2-aminoethyl)pyridine; D000242:Cyclic AMP; D011494:Protein Kinases; D013890:Thiourea; D017259:Dimaprit