SCH 28080 is a more selective inhibitor than SCH 32651 at the K+ site of gastric K+/H+-ATPase.

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作者信息

Beil W, Staar U, Sewing K F

机构信息

Abteilung Allgemeine Pharmakologie, Medizinische Hochschule Hannover, F.R.G.

出版信息

Eur J Pharmacol. 1987 Jul 23;139(3):349-52. doi: 10.1016/0014-2999(87)90593-0.

DOI:10.1016/0014-2999(87)90593-0

PMID:2822435

Abstract

The anti-secretory agents SCH 32651 and SCH 28080 were compared for their potency to interact with the K+ site of guinea-pig parietal cell K+/H+-ATPase and dog kidney Na+/K+-ATPase. SCH 32651 and SCH 28080 had an inhibition constant of 9.0 and 0.02 mumol/l, respectively, for the K+/H+-ATPase. The Ki values for the Na+/K+-ATPase were 140 and 220 mumol/l. The data show that both drugs have a higher affinity to the K+ site of the K+/H+-ATPase than to that of the Na+/K+-ATPase and that the affinity ratio of SCH 28080 in favour of K+/H+-ATPase is much greater (11,000) than that of SCH 32651 (15).

摘要