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Physico-Chemical Studies of β-Adrenergic Receptors on Intact Cells

  • Johan Hoebeke
  • A. Donny Strosberg
Part of the Methodological Surveys in Biochemistry and Analysis book series (MSBA, volume 13)

Abstract

Kinetic studies were performed on intact murine cells using 3H-dihydroalprenolol as antagonist and 3H-hydroxybenzylisoproterenol as agonist radioligands for the β-adrenergic receptor. The binding specificity was tested by inhibition of binding of the radiolabeled antagonist by the agonist 1-isoproterenol and of the radiolabeled agonist by the antagonist dl-alprenolol.

The kinetics of the antagonist association are compatible with a diffusion-controlled process. Dissociation of the antagonist showed a biphasic Arrhenius plot with a low activation energy at temperatures under 20° and a 10-fold increase in activation energy above this temperature. The agonist did not bind specifically below 20°. Above 20° the binding kinetics reflect the need for a conformational change in the receptor before tight binding of agonist can occur.

Keywords

Arrhenius Plot Binding Kinetic Agonist Binding Dissociation Rate Constant Association Rate Constant 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Plenum Press, New York 1984

Authors and Affiliations

  • Johan Hoebeke
    • 1
  • A. Donny Strosberg
    • 1
  1. 1.Laboratory of Molecular Immunology, Institut Jacques Monod, C.N.R.S.Université Paris VIIParis Cedex 05France

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