title: Histamine receptor effects on dissipation of an intracellular proton gradient of isolated gastric mucosal surface cells.
abstract: The effects of histamine and several H1 and H2 receptor agents on Na+/H+ and Cl-/HCO-3 exchange systems of isolated gastric mucosal surface cells were studied. The cells were acid-loaded by the NH4Cl prepulse technique and the spontaneous Na+- and HCO-3-induced dissipation of the intracellular proton gradient (pHi) was followed using the metachromatic dye acridine orange. Histamine (10(-2-5) M) stimulates HCO-3-induced dissipation of the pHi but has no effect on Na+-induced or spontaneous dissipation. The H1 agonist 2-(2-aminoethyl)pyridine and the H2 agonist dimaprit also have no effect on Na+-induced or spontaneous pHi dissipation. However, both of these agents mimic the effect of histamine on HCO-3-induced dissipation, but only at a higher concentration (10(-3) M). The combination of 2-(2-aminoethyl)pyridine and dimaprit produces a histamine-like effect at lower concentrations (10(-5) and 10(-4) M). The effects of histamine are blocked by either the H1 antagonists diphenhydramine and pyrilamine or the H2 antagonists cimetidine and SKF 93479. The results suggest that the effect of histamine on HCO-3-induced dissipation of a pHi in gastric mucosal surface cells is mediated through a coordinated mechanism involving both H1 and H2 receptor sites.
mesh_terms: D000818:Animals; D001639:Bicarbonates / Q000378:metabolism / Q000494:pharmacology; D002712:Chlorides / Q000378:metabolism; D002927:Cimetidine / Q000494:pharmacology; D017259:Dimaprit; D004155:Diphenhydramine / Q000494:pharmacology; D005744:Gastric Acid / Q000378:metabolism*; D005753:Gastric Mucosa / Q000187:drug effects / Q000502:physiology*; D006632:Histamine / Q000494:pharmacology; D011522:Protons; D011725:Pyridines / Q000494:pharmacology; D011738:Pyrilamine / Q000494:pharmacology; D011817:Rabbits; D011968:Receptors, Histamine / Q000502:physiology*; D011969:Receptors, Histamine H1 / Q000502:physiology*; D011970:Receptors, Histamine H2 / Q000502:physiology*; D012964:Sodium / Q000378:metabolism / Q000494:pharmacology; D013890:Thiourea / Q000494:pharmacology
chemical_list: D001639:Bicarbonates; D002712:Chlorides; D011522:Protons; D011725:Pyridines; D011968:Receptors, Histamine; D011969:Receptors, Histamine H1; D011970:Receptors, Histamine H2; D002927:Cimetidine; D006632:Histamine; D004155:Diphenhydramine; D012964:Sodium; C006183:2-(2-aminoethyl)pyridine; D013890:Thiourea; D011738:Pyrilamine; D017259:Dimaprit