Evidence against the "spare" receptor nature of alpha 2-adrenoceptors in hamster white fat cells

Biochem Int. 1990;20(4):779-86.

Abstract

After having established the alpha 2-adrenoceptor nature of the binding sites specifically labeled by the alpha 2-agonist [3H] UK 14304 in hamster adipocytes, two different approaches have been used to determine whether these alpha 2-adrenoceptors were "spare receptors". The first one, consisted to block irreversibly fractions of the receptor population by various concentrations of the alpha 2-antagonist benextramine and determine the relationship between the residual receptor occupancy by UK 14304 and the corresponding magnitude of the cellular inhibitory cyclic AMP response to the alpha 2-adrenergic component of epinephrine under conditions avoiding cyclic AMP breakdown. The second approach was a detailed comparison between alpha 2-receptor occupancy by [3H] UK 14304 and the cyclic AMP inhibitory dose-response curve to this agonist in cells incubated also under conditions avoiding cyclic AMP breakdown. These two experimental approaches clearly showed that the alpha 2-adrenoceptor of hamster adipocytes are not "spare receptors".

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adipose Tissue / metabolism*
  • Adrenergic alpha-Antagonists / pharmacology
  • Animals
  • Binding Sites
  • Binding, Competitive
  • Brimonidine Tartrate
  • Cell Membrane / metabolism
  • Cricetinae
  • Cyclic AMP / metabolism
  • Cystamine / pharmacology
  • Kinetics
  • Male
  • Mesocricetus
  • Quinoxalines / metabolism
  • Receptors, Adrenergic, alpha / metabolism*

Substances

  • Adrenergic alpha-Antagonists
  • Quinoxalines
  • Receptors, Adrenergic, alpha
  • Brimonidine Tartrate
  • benextramine
  • Cyclic AMP
  • Cystamine