Inhibition of bone resorption by H+/K+-ATPase inhibitors

R Sarges, A Gallagher, TJ Chambers…

Index: Sarges, Reinhard; Gallagher, Andrea; Chambers, Timothy J.; Yeh, Li-An Journal of Medicinal Chemistry, 1993 , vol. 36, # 19 p. 2828 - 2830

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Citation Number: 39

Abstract

We have found that 3-(3-(ethoxycarbonyl) propionyl)-8-methoxy-4-((2-methylpheny1) amino) quin-oline (1, CP-113,411), a reversible inhibitor of gastric H+/K+-ATPase (IC50 10-20 mM), is also a potent inhibitor of bone resorption by osteoclasts in a bone slice assay at concentrations as low as M, with an IC50 of 2 mM. By contrast, the structurally related H+/K+- ATPase inhibitor 2 (3-(ethoxycarbonyl)-8-methoxy-4-((2-methylphenyl) amino) quinoline) ...