Effect of polyamine related tetraamines on anti-ulcerogenic activity and anti-H+,K+-ATPase activity.

The relationship between the structure of polyamine related tetraamines and their anti-ulcerogenic activity in rats was studied. Among the tetraamines tested, linear tetraamines had stronger anti-ulcerogenic activity in both restraint stress-induced gastric ulceration and ulceration in pylorus-ligated rats. Macrocyclic tetraamines and polycyclotetraamines had less anti-ulcerogenic activity. Correlation was detected between the inhibitory effect of tetraamines on gastric secretion in pylorus-ligated rats and their inhibitory effect on H+,K+-ATPase activity in rat gastric mucosa. Thermine and spermine were the most effective in these two inhibitions. Thus, it is suggested that primary aminogroups are important in both anti-ulcerogenic activity and anti-H+,K+-ATPase activity.