AU-461 is a reversible inhibitor of the gastric H⁺/K⁺ ATPase, exhibiting IC₅₀ values of 12.15 μM for rabbit-derived enzymes and 4.20 μM for pig-derived enzymes. By competing with activated cationic K⁺ (Kᵢ = 1.64 μM), AU-461 effectively reduces both histamine-stimulated and basal gastric acid secretion in rat models. This compound demonstrates protective effects against ulcer formation induced by ethanol or sodium hydroxide and normalizes plasma gastrin levels. AU-461 is valuable for research into the mechanisms of peptic ulcers and gastric acid regulation.
AU-461 is a reversible inhibitor of the gastric H⁺/K⁺ ATPase, exhibiting IC₅₀ values of 12.15 μM for rabbit-derived enzymes and 4.20 μM for pig-derived enzymes. By competing with activated cationic K⁺ (Kᵢ = 1.64 μM), AU-461 effectively reduces both histamine-stimulated and basal gastric acid secretion in rat models. This compound demonstrates protective effects against ulcer formation induced by ethanol or sodium hydroxide and normalizes plasma gastrin levels. AU-461 is valuable for research into the mechanisms of peptic ulcers and gastric acid regulation.
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