title: Pharmacological control of the histamine H2 receptor-adenylate cyclase system by famotidine and ranitidine in normal and cancerous human gastric epithelia.
abstract: In human fundic glands, famotidine was about 17 times more potent than ranitidine as an inhibitor of histamine - stimulated cAMP generation. This H2-receptor antagonist had no effect on the receptor-adenylate cyclase systems sensitive to PGE2, isoproterenol (beta 2-receptor), VIP and on forskolin-induced activation of the Gs/catalytic units of the membrane-bound enzyme prepared from human fundic glands. In the HGT-1 human gastric cancer cell line, famotidine and ranitidine showed long lasting, irreversible actions probably related to a slow rate of dissociation from the histamine H2-receptor.
authors.affiliation: INSERM U.55, Hôpital Saint-Antoine, Paris, France.
authors.forename: D
authors.initials: D
authors.lastname: Fagot
authors.forename: S
authors.initials: S
authors.lastname: Emami
authors.forename: E
authors.initials: E
authors.lastname: Chastre
authors.forename: W
authors.initials: W
authors.lastname: Bawab
authors.forename: C
authors.initials: C
authors.lastname: Gespach
mesh_terms: D000262:Adenylyl Cyclases / Q000378:metabolism; D004848:Epithelium / Q000187:drug effects / Q000378:metabolism; D015738:Famotidine; D005748:Gastric Fundus / Q000187:drug effects* / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D011899:Ranitidine / Q000494:pharmacology*; D011970:Receptors, Histamine H2 / Q000187:drug effects; D013274:Stomach Neoplasms / Q000378:metabolism; D013844:Thiazoles / Q000494:pharmacology*
chemical_list: D011970:Receptors, Histamine H2; D013844:Thiazoles; D015738:Famotidine; D011899:Ranitidine; D000262:Adenylyl Cyclases