PMID: 9165692May 1, 1996Paper

Current status of acid pump antagonists (reversible PPIs)

The Yale Journal of Biology and Medicine
W Wurst, M Hartmann

Abstract

The introduction of H2-receptor antagonists in the mid-1970s provided, for the first time, acceptable medical therapy for acid-related diseases. Their short duration of action and single receptor targeting, however, limited satisfactory treatment of patients. Today the control of gastric acid secretion can be effectively achieved by direct inhibition of the H+, K(+)-ATPase. Inhibition of the proton pump suppresses acid secretion independent of the route of stimulation. Two classes of drugs are able to inhibit the proton pump. First, the substituted benzimidazoles (proton pump inhibitors [PPIs]), which, due to their pKa of about 4, accumulate in the acidic secretory canaliculus of the stimulated parietal cell. Following conversion to a cationic sulfenamide, they react with cysteines on the extracytoplasmatic face of the H+, K(+)-ATPase subunit. Second, acid pump antagonists (APAs) acting by K(+)-competitive and reversible binding to the gastric proton pump, which is the final step for activation of acid secretion in the parietal cell. One possible class of APAs are imidazopyridines. BY841 was selected from this class and is chemically a (8-(2-methoxycarbonylamino-6-methyl-phenylmethylamino )-2,3-dimethyl-imidazo [1,2-a]-pyridine...Continue Reading

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