title: Studies on antiulcer agents. II. Antiulcer properties of N-(1H-tetrazol-5-yl)-2-anilino-5-pyrimidinecarboxamides inhibiting release of histamine from passively sensitized rat peritoneal mast cells.
abstract: With the aim of applying mast cell-stabilizing agents as antiulcer agents, N-(1H-tetrazol-5-yl)-2-anilino-5-pyrimidinecarboxamides were synthesized, and initially evaluated pharmacologically for activity in the rat passive cutaneous anaphylaxis test by oral administration. The most active compound 6 was proved to inhibit potently the release of histamine from passively sensitized rat peritoneal mast cells in vitro. When compared with other mast cell-stabilizing agents and an antiulcer agent, compound 6 was found to show excellent gastric mucosal protection and gastric antisecretion activities. Furthermore, compound 6 revealed good activity against acidified aspirin ulcer in rats and water-immersion stress ulcer in rats.
authors.affiliation: Research Laboratories, Roussel Morishita Co., Ltd., Shiga, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Terashima
authors.forename: T
authors.initials: T
authors.lastname: Tanimura
authors.forename: H
authors.initials: H
authors.lastname: Shimamura
authors.forename: A
authors.initials: A
authors.lastname: Kawase
authors.forename: K
authors.initials: K
authors.lastname: Uenishi
authors.forename: Y
authors.initials: Y
authors.lastname: Tanaka
authors.forename: I
authors.initials: I
authors.lastname: Kimura
authors.forename: T
authors.initials: T
authors.lastname: Kamisaki
authors.forename: Y
authors.initials: Y
authors.lastname: Ishizuka
authors.forename: M
authors.initials: M
authors.lastname: Sato
mesh_terms: D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001241:Aspirin; D002927:Cimetidine / Q000494:pharmacology; D004205:Cromolyn Sodium / Q000494:pharmacology; D000431:Ethanol; D006634:Histamine H1 Antagonists / Q000494:pharmacology; D006636:Histamine Release / Q000187:drug effects*; D008407:Mast Cells / Q000187:drug effects / Q000378:metabolism*; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D010529:Peritoneal Cavity / Q000166:cytology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013276:Stomach Ulcer / Q000139:chemically induced / Q000188:drug therapy; D013777:Tetrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D062367:ortho-Aminobenzoates / Q000494:pharmacology
chemical_list: D000897:Anti-Ulcer Agents; D006634:Histamine H1 Antagonists; D011743:Pyrimidines; D013777:Tetrazoles; D062367:ortho-Aminobenzoates; D000431:Ethanol; D002927:Cimetidine; C012293:tranilast; D004205:Cromolyn Sodium; D001241:Aspirin