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Picoprazole is a specific inhibitor of H+/K+-ATPase with IC50 of 3.1±0.4 μM.

Picoprazole inhibits the H+/K+-ATPase activity in a concentration-dependent manner. The IC50 value is 3.1±0.4 μM[1]. Picoprazole is a specific inhibitor of H+/K+-ATPase and binds to 100-kDa polypeptides of the enzyme, dose dependently inhibited opening of the Cl- conductance by Cu2+-o-phenanthroline, indicating that the Cl- conductance is part of the function of the H+/K+-ATPase[2]. The inhibitory effect of the three benzimidazole derivatives Timoprazole, Picoprazole, and Omeprazole on histamine and dbcAMP stimulated 14C-aminopyrine accumulation (H+ secretion) has been studied in isolated and enriched guinea-pig parietal cells. All compounds tested inhibit H+ secretion in a concentration dependent manner with IC50 values of 8.5±1.9 μM for Timoprazole, 3.9±0.7 μM for Picoprazole, and 0.13±0.03 μM for Omeprazole[3].

[1]. Beil W, et al. Inhibition of partially purified H+/K+-ATPase from guinea-pig isolated and enriched parietal cells by substituted benzimidazoles. Br J Pharmacol. 1984 Jul;82(3):651-7. [2]. Takeguchi N, et al. Disulfide cross-linking of H,K-ATPase opens Cl- conductance, triggering proton uptake in gastric vesicles. Studies with specific inhibitors. J Biol Chem. 1986 Feb 25;261(6):2560-6. [3]. Sewing KF, et al. Effect of substituted benzimidazoles on acid secretion in isolated and enriched guinea pig parietal cells. Gut. 1983 Jun;24(6):557-60.

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