Mechanism of action of AZD0865, a K+-competitive inhibitor of gastric H+,K+-ATPase.

@article{Gedda2007MechanismOA,
  title={Mechanism of action of AZD0865, a K+-competitive inhibitor of gastric H+,K+-ATPase.},
  author={Karin Gedda and Carin Briving and Karin Svensson and Ingela Maxvall and Kjell Andersson},
  journal={Biochemical pharmacology},
  year={2007},
  volume={73 2},
  pages={198-205}
}
AZD0865 is a member of a drug class that inhibits gastric H(+),K(+)-ATPase by K(+)-competitive binding. The objective of these experiments was to characterize the mechanism of action, selectivity and inhibitory potency of AZD0865 in vitro. In porcine ion-leaky vesicles at pH 7.4, AZD0865 concentration-dependently inhibited K(+)-stimulated H(+),K(+)-ATPase activity (IC(50) 1.0+/-0.2 microM) but was more potent at pH 6.4 (IC(50) 0.13+/-0.01 microM). The IC(50) values for a permanent cation… CONTINUE READING

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