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.
View Article and Find Full Text PDFEksp Klin Farmakol
June 1995
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.
View Article and Find Full Text PDFThe effects of some antiallergic drugs on H1-histamine, 5-HT2-serotonin, and M-cholinoreceptors ligand binding in the rat brain were studied in vitro. Dimedrol, dimebon, and phencarol bonded to H1-receptors: IC50 were 76 +/- 10, 153 +/- 15, 320 +/- 60 nM, respectively. Diazoline and dimebon had some affinity for 5-HT2-receptors, its IC50 was 880 +/- 90 nM.
View Article and Find Full Text PDFThe effect of an antiallergic (antihistaminic and antiserotonin) drug bicarphen on the functional state of the central nervous system (CNS) was studied. In experiments on animals bicarphen in contrast to dimedrol (diphenhydramine) exerted predominantly the activating effect on CNS (decreased the hypnotic action of barbamyl, enhanced the summation capacity of CNS and the activity of mice in the escape behavioral test, increased the bioelectrical activity of the brain and the activating effect of antidepressants on the EEG).
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