Desensitization by histamine of H2 receptor-mediated adenylate cyclase activation in the human gastric cancer cell line HGT-1.
Short-term treatment of cultured HGT-1 cells with histamine produced a time-dependent (half-life: 20 min) and homologous desensitization of histamine H2 receptor activity mediating cAMP generation in HGT-1 cells and gastric acid secretion in normal gastric mucosa. Histamine treatment resulted in loss of response of the adenylate cyclase to histamine in purified plasma membranes, but had no effect on basal, vasoactive intestinal peptide (VIP)- or NaF-stimulated enzyme activities. We propose that the desensitization of gastric histamine H2 receptor by histamine evidenced in cellular or subcellular preparations from HGT-1 cells could be involved in the physiological regulation and pharmacological control of gastric cell function in man.
D000262:Adenylyl Cyclases / Q000378:metabolism*; D002460:Cell Line; D002462:Cell Membrane / Q000201:enzymology; D000242:Cyclic AMP / Q000502:physiology; D004789:Enzyme Activation; D006632:Histamine / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D011968:Receptors, Histamine / Q000502:physiology*; D011970:Receptors, Histamine H2 / Q000502:physiology*; D013274:Stomach Neoplasms / Q000201:enzymology*
D011968:Receptors, Histamine; D011970:Receptors, Histamine H2; D006632:Histamine; D000242:Cyclic AMP; D000262:Adenylyl Cyclases