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J. Biol. Chem., Vol. 262, Issue 5, 2077-2084, Feb, 1987
B Wallmark, C Briving, J Fryklund, K Munson, R Jackson, J Mendlein, E Rabon and G Sachs
A hydrophobic amine, SCH 28080, 2-methyl-8-
(phenylmethoxy)imidazo(1,2a)pyridine-3-acetonitrile, previously shown to
inhibit gastric acid secretion in vivo and in vitro, was also shown to
inhibit basal and stimulated aminopyrine accumulation in isolated gastric
glands when histamine, high K+ concentrations, or dibutyryl cAMP were used
as secretagogues. Stimulated, but not basal, oxygen consumption was also
inhibited. Neutralization of the acid space of the parietal cell by high
concentrations of the weak base, imidazole, reduced the potency of the
drug, suggesting that SCH 28080 was active when protonated. Studies on the
isolated H+,K+-ATPase showed that the compound inhibited the enzyme
competitively with K+, whether ATP or p- nitrophenyl phosphate were used as
substrates. In contrast, the inhibition was mixed with respect to
p-nitrophenyl phosphate and uncompetitive with respect to ATP. The drug
reduced the steady state level of the phosphoenzyme but not the observed
rate constant for phosphoenzyme formation in the absence of K+ nor the
quantity of phosphoenzyme reacting with K+. The drug quenched the
fluorescence of fluorescein isothiocyanate-modified enzyme and also
inhibited the ATP- independent K+ exchange reaction of the H+,K+-ATPase.
Its action on gastric acid secretion can be explained by inhibition of the
H+,K+- ATPase by reversible complexation of the enzyme. This class of
compound, therefore, acts as a reversible inhibitor of gastric acid
secretion.
Inhibition of gastric H+,K+-ATPase and acid secretion by SCH 28080, a substituted pyridyl(1,2a)imidazole
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