H<SUP>+</SUP>/K<SUP>+</SUP>-ATPase阻害剤
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Gastric H<SUP>+</SUP>/K<SUP>+</SUP>-ATPase, located in the parietal cell, is responsible for the final step of acid secretion in the stomach. Since omeprazole, a sulfinyl compound, was found to inhibit H<SUP>+</SUP>/K<SUP>+</SUP>-ATPase in 1983, there has been considerable interest in H<SUP>+</SUP>/K<SUP>+</SUP>-ATPase inhibitor as a splendid drug for the treatment of peptic ulcer. H<SUP>+</SUP>/K<SUP>+</SUP>-ATPase inhibitors are classified into two categories. One is an irreversible inhibitor binding to a critical thiol group on the enzyme, such as omeprazole, lansoprazole and NC-1300-O-3, and the other is a reversible K<SUP>+</SUP>-competitive inhibitor. In the former, substituted pyridyl derivatives transform in the acid compartments of the parietal cell into the active inhibitor. This paper reviews the development of H<SUP>+</SUP>/K<SUP>+</SUP>-ATPase inhibitors.
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