The binding of [3H]R‐PIA to A1 adenosine receptors produces a conversion of the high‐ to the low‐affinity state
Open Access
- 29 July 1991
- journal article
- research article
- Published by Wiley in FEBS Letters
- Vol. 286 (1-2) , 221-224
- https://doi.org/10.1016/0014-5793(91)80978-c
Abstract
Kinetic evidence for negative cooperativity on the binding of [3H]R-PIA to A1 adenosine receptors was obtained from dissociation experiments at different ligand concentrations and from the equilibrium isotherm. The dissociation curves indicate that there is an apparent ligand-induced transformation of high- to low-affinity states of the receptor. At concentrations of 18.2 nM R-PIA or higher there was only found the low-affinity state of the receptor. In view of these results equilibrium binding data were analyzed by the usual two-state model (assuming that there is an interconversion between them) and by the negative cooperativity model employing the Hill equation.Keywords
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