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.
Kakegawa
T
T
Faculty of Pharmaceutical Sciences, Chiba University, Japan.
Hirose
S
S
Kimura
E
E
Aihara
H
H
Isobe
Y
Y
Igarashi
K
K
D000251:Adenosine Triphosphatases / Q000037:antagonists & inhibitors*; D000818:Animals; D000897:Anti-Ulcer Agents; D005744:Gastric Acid / Q000378:metabolism; D017506:H(+)-K(+)-Exchanging ATPase; D006632:Histamine / Q000494:pharmacology; D008297:Male; D008861:Microsomes / Q000187:drug effects / Q000378:metabolism; D011073:Polyamines / Q000494:pharmacology*; D011708:Pylorus / Q000502:physiology; D051381:Rats; D011919:Rats, Inbred Strains; D012149:Restraint, Physical; D013096:Spermine / Q000494:pharmacology; D013276:Stomach Ulcer / Q000188:drug therapy* / Q000209:etiology; D013315:Stress, Psychological / Q000150:complications
D000897:Anti-Ulcer Agents; D011073:Polyamines; D013096:Spermine; D006632:Histamine; D000251:Adenosine Triphosphatases; D017506:H(+)-K(+)-Exchanging ATPase