AN INVESTIGATION OF ANTIHISTAMINIC ACTIVITY AND GASTRIC ULCERATION

An investigation of antihistaminic activity and gastric ulceration has been done in guinea pigs and rats. Gastric ulcers were produced in guinea pigs by histamine and restraint procedures, while pyloric-ligation and reserpine were used in rat experiments. Brompheniramine, AHR-224-B, tripelenamine HCl, cyproheptadine HCl and promethazine HCl were effective in preventing histamine-induced ulceration in guinea pigs. Glycopyrrolate, a potent anticholinergic, was ineffective. Brompheniramine, the most potent antihistamine (against histamine-induced ulceration), was further investigated for its effects on gastric ulceration induced by other procedures. In restraint-induced ulcers in guinea pigs, the drug was without protective effect. When the gastric ulceration was produced in rats by pyloric-ligation or reserpine, this antihistamine, in contrast to glycopyrrolate, did not exert a protective action. These studies show that several antihistamines are effective antagonists to histanine-induced gastric ulceration in guinea pigs. The effectiveness of certain pharmacological agents (antihistamine or anticholinergic) in preventing gastric ulceration is determined to a large degree by the method employed to produce the ulceration. © 1969.