Bl. Slomiany et al., ENHANCEMENT OF GASTRIC MUCUS PHOSPHOLIPID SECRETION BY AN ANTIULCER AGENT, EBROTIDINE, General pharmacology, 25(5), 1994, pp. 1033-1037
1. Rat gastric mucosal cells, subjected to phospholipid labeling by in
cubating the cell suspension in DR?EM with [H-3]choline, were exposed
to different concentrations (0-150 mu M) of H-2-receptor antagonists,
ebrotidine and ranitidine, and the phospholipid secretory responses we
re evaluated. 2. In the absence of the drugs, the secretion of choline
-containing phospholipids over a I hr period averaged 3.97% of the tot
al cellular labeled phospholipids. Ebrotidine caused a dose-dependent
increase in the rate of phospholipid secretion which was most pronounc
ed at 1 hr and persisted for at least 2 hr. The maximal effect was att
ained at 120 mu M ebrotidine giving a 36% increase in phospholipid sec
retion. 3. The phospholipid secretory response to ebrotidine was accom
panied by an increase in gastric mucosal cell cAMP level which reached
a maximum value of 2.1-fold over that of controls at 1 hr. Ranitidine
, in contrast, neither evoked increase in cAMP level nor caused any st
imulation in phospholipid secretion. 4. The results indicate that the
gastroprotective properties of ebrotidine are associated with the abil
ity of the drug to elicit a rapid stimulation in gastric mucus phospho
lipid secretion, and that ranitidine does not possess such property.