[Studies on the intracellular pharmacodynamic properties of proton pump inhibitors and the inhibitory mechanism of acid secretion].
In recent studies, proton pump inhibitors, such as omeprazole, were found to be transformed into sulfenamide derivatives in the acid space of isolated parietal cells. It is considered that these sulfenamide derivatives mainly inhibit H+, K(+)-ATPase activity. To clarify the inhibitory mechanism of proton pump inhibitors, we studied the effect on acid secretion of the isolated parietal cells. Proton pump inhibitors inhibited histamine-, carbachol- and gastrin-stimulated 14C-aminopyrine accumulation. Db-cAMP stimulation was also inhibited by these inhibitors. Consequently, it is believed that the origin of H+, K(+)-ATPase was located in the final stage of the acid production.
Saito
E
E
Third Department of Internal Medicine, Faculty of Medicine, University of Tokyo.
Matsuo
Y
Y
D000251:Adenosine Triphosphatases / Q000037:antagonists & inhibitors*; D000632:Aminopyrine / Q000493:pharmacokinetics; D000818:Animals; D002217:Carbachol / Q000037:antagonists & inhibitors; D002478:Cells, Cultured; D000242:Cyclic AMP / Q000037:antagonists & inhibitors; D003864:Depression, Chemical; D005744:Gastric Acid / Q000378:metabolism*; D017506:H(+)-K(+)-Exchanging ATPase; D006633:Histamine Antagonists; D006801:Humans; D009853:Omeprazole / Q000493:pharmacokinetics / Q000494:pharmacology*; D010295:Parietal Cells, Gastric / Q000378:metabolism
D006633:Histamine Antagonists; D000632:Aminopyrine; D002217:Carbachol; D000242:Cyclic AMP; D000251:Adenosine Triphosphatases; D017506:H(+)-K(+)-Exchanging ATPase; D009853:Omeprazole