ABSTRACT
A series of four new furoxanopyrimidine derivatives was synthesized and studied with respect to antiulcerous, antisecretory, and antibacterial activity. Two compounds exhibit antiulcerous effect not accompanied (in contrast to the well-known H2 receptor blockers, quiditene, and other antiulcerous drugs) by inhibition of gastric acid secretion. No one of the studied compounds exhibited antibacterial activity in the tests with Helicobacter pylori.
Subject(s)
Anti-Ulcer Agents/therapeutic use , Oxadiazoles/pharmacology , Pyrimidines/pharmacology , Stomach Ulcer/drug therapy , Animals , Dose-Response Relationship, Drug , Gastric Mucosa/drug effects , Gastric Mucosa/metabolism , Helicobacter pylori/drug effects , Male , Nitric Oxide Donors/pharmacology , Rats , Stomach Ulcer/chemically induced , Stomach Ulcer/physiopathologyABSTRACT
Quiditene-(qunuclidyl-3)-di-(thyenel-2)carbinole hydrochloride was studied by using various experimental models. The agent was compared with H2-blockers. When gastrically used, quiditene in doses of 5-50 mg/kg dose-dependently decreased gastric acid secretion and prevented acute gastric mucosal lesions. As cimetidine and ranitidine, the agent accelerated chronic gastric ulcer healing. Quiditene has been allowed for clinical studies in Russia.
Subject(s)
Anti-Ulcer Agents/pharmacology , Gastric Mucosa/metabolism , Quinuclidines/pharmacology , Animals , Anti-Ulcer Agents/therapeutic use , Chronic Disease , Cimetidine/pharmacology , Cimetidine/therapeutic use , Drug Evaluation, Preclinical , Gastric Mucosa/drug effects , Mice , Quinuclidines/therapeutic use , Ranitidine/pharmacology , Ranitidine/therapeutic use , Rats , Stomach Ulcer/chemically induced , Stomach Ulcer/drug therapy , Stomach Ulcer/etiology , Stress, Physiological/complications , Time FactorsABSTRACT
Experiments were made to study the influence of a new antihistaminic drug phencarol [(quinuclidyl-3) diphenylcarbinol hydrochloride] on gastric secretion in rats. Unlike the blockers of H1-histamine receptors (diphenhydramine, omeril, pyrilamine, and cyproheptadine), phencarol reduces secretion and the content of free hydrochloric acid in the gastric contents. The antacid activity of the drug is similar to that of the H2-receptor blocker, cimetidine. However, phencarol differs from the latter drug in the mechanism of action. The antacid action of phencarol is likely to be the result of its activation effect on diamine oxidase, which leads to a decrease in the content of active histamine in the tissues and diminution of its supply to H2-histamine receptors that control gastric secretion.
Subject(s)
Gastric Mucosa/metabolism , Histamine H1 Antagonists/pharmacology , Animals , Benzhydryl Compounds/pharmacology , Carbolines/pharmacology , Cimetidine/pharmacology , Cyproheptadine/pharmacology , Diphenhydramine/pharmacology , Male , Pyrilamine/pharmacology , RatsABSTRACT
Effect of a new antidepressant pyrazidol (1,10-trimethylene-8-methyl-1,2,3,4-tetrahydropyrazino /1,2-/ indole) on the liver and brain MAO activity of rats was studied in experiments in vivo and in vitro. Pyrazidol selectively blocks type A MAO (the substrates serotonin and noradrenaline) and does not virtually affect or has a far less action on type B MAO (the substrate 2-phenylethylamine).
