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• W1993670887 abstract "Ouabain binding was studied in isolated adult dog heart myocytes. The binding was correlated with the inhibition of K+-activated para-nitrophenylphosphatase (K+-PNPPase) activity and the beating response. It was shown that: (i) the specific binding was dependent upon Mg2+ and was inhibited by K+; (ii) the maximal binding capacity (Bmax) was 7.4 × 105 ouabain molecules per cell, or 410 pmol ouabain/K+-PNPPase unit (μmol/min); (iii) in the presence of Mg2+ (5 mm), there were two components in the Scatchard plot, i.e., a high-affinity component with a Kd value of 5.6 × 10−8m and a low-affinity component with a Kd value of 6.7 × 10−7m; (iv) the Hill coefficient (n′) for ouabain binding was 0.72 with a S0.5 value of 7.1 × 10−7m; these values were compatible with the values obtained from studies of K+-PNPPase inhibition by ouabain (n′ = 0.55, S0.5 = 3.6 × 10−7 m) and remained unchanged in the presence of physiological concentrations of Na+ plus K+; (v) in the presence of Mg2+ and K+, the high-affinity component tended to conform to the low-affinity component with an apparent decrease in Bmax; (vi) in the presence of Mg2+ and para-nitrophenylphosphate, the low-affinity component was changed to the high-affinity component with no change in Bmax; (vii) the dissociation rate of the labeled ouabain in the highly dilute medium was not altered in the presence of excess amounts of unlabeled ligand; this eliminated the possibility that the apparent negative cooperativity was due to a site-to-site interaction between receptors; (viii) ouabain increased the number of beating cells and the frequency of beating. Based on these findings, it is concluded that: (i) isolated myocytes possess functional receptors for ouabain; (ii) the binding of ouabain is associated with its inhibition of K+-PNPPase activity; (iii) ouabain receptors in isolated myocytes are of one class with at least two interconvertible conformational states." @default.
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• W1993670887 date "1981-03-01" @default.
• W1993670887 modified "2023-10-04" @default.
• W1993670887 title "Ouabain receptor in isolated adult dog heart myocytes" @default.
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• W1993670887 doi "https://doi.org/10.1016/0003-9861(81)90020-5" @default.
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