STUDIES ON ANTIULCER AGENTS .2. ANTIULCER PROPERTIES OF -TETRAZOL-5-YL)-2-ANILINO-5-PYRIMIDINECARBOXAMIDES INHIBITING RELEASE OF HISTAMINE FROM PASSIVELY SENSITIZED RAT PERITONEAL MAST-CELLS

With the aim of applying mast cell-stabilizing agents as antiulcer age nts, -tetrazol-5-yl)-2-anilino-5-pyrimidinecarboxamides were synthesiz ed, and initially evaluated pharmacologically for activity in the rat passive cutaneous anaphylaxis test by oral administration. The most ac tive compound 6 was proved to inhibit potently the release of histamin e from passively sensitized rat peritoneal mast cells in vitro. When c ompared with other mast cell-stabilizing agents and an antiulcer agent , compound 6 was found to show excellent gastric mucosal protection an d gastric antisecretion activities. Furthermore, compound 6 revealed g ood activity against acidified aspirin ulcer in rats and water-immersi on stress ulcer in rats.