SCH 28080 is a more selective inhibitor than SCH 32651 at the K+ site of gastric K+/H+-ATPase
| Autor: | Karl-Fr. Sewing, Ute Staar, Winfried Beil |
|---|---|
| Rok vydání: | 1987 |
| Předmět: |
Stereochemistry
ATPase Guinea Pigs In Vitro Techniques Kidney H(+)-K(+)-Exchanging ATPase Dogs polycyclic compounds medicine Potency Animals heterocyclic compounds Na+/K+-ATPase Inhibition constant Parietal cell Pharmacology Adenosine Triphosphatases biology Chemistry organic chemicals Imidazoles Anti-Ulcer Agents carbohydrates (lipids) Kinetics medicine.anatomical_structure nervous system Mechanism of action Enzyme inhibitor Gastric Mucosa Pyrazines biology.protein Potassium medicine.symptom Sodium-Potassium-Exchanging ATPase Site of action |
| Zdroj: | European journal of pharmacology. 139(3) |
| ISSN: | 0014-2999 |
| Popis: | 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 μmol/1, respectively, for the K + /H + -ATPase. The K i values for the Na + /K + -ATPase were 140 and 220 μmol/1. 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). |
| Databáze: | OpenAIRE |
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