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  • Title: Modulatory effect of some steroid hormones, their glucuronides and ouabain-like compounds on Cavia cobaya kidney Na+,K(+)-ATPase activity.
    Author: Giunta C, Ferrero P, Pizzuto M, Cavaletto M, Pessione E, Bracchino P.
    Journal: Gen Pharmacol; 1990; 21(4):435-42. PubMed ID: 2165954.
    Abstract:
    1. Ouabain-like compounds (approx. mol. wt 700, 2,000 and 4,000 Da) were purified from plasma of essential hypertensive patients. 2. Dose-response experiments performed with (a) steroid hormones, (b) their glucuronides and (c) ouabain-like compounds, emphasize a modulatory effect [activation of the Na,K-ATPase at very low concentrations of ligand, inhibition at higher levels; apparent Ki: (a) between 1 and 0.5 mM; (b) between 1 and 0.5 microM; and (c) between 10 and 1 nM; maximum enhancement of the enzymatic activity: (a) +20%; (b) +45%; and (c) +100%]. 3. Displacement experiments of [3H]ouabain evidence a high competition of the ligands towards the cardioglycoside. The relative I50s are: (a) between 1 and 0.5 mM; (b) between 10 and 1 microM; and (c) between 10 and 0.01 nM.
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