Radioligand binding studies of the atypical beta 3-adrenergic receptor in rat brown adipose tissue using [3H]CGP 12177

FEBS Lett. 1992 Feb 24;298(2-3):162-4. doi: 10.1016/0014-5793(92)80046-j.

Abstract

Two populations of [3H]CGP 12177 binding sites exist in rat interscapular brown adipose tissue (IBAT) plasma membranes. The majority of binding sites are of low affinity with a Kd of 31 nM, a value in close agreement with that for the Kd of [3H]CGP 12177 binding to a cloned rat beta 3-adrenergic receptor (AR) expressed in CHO cells (44 nM). Competition binding studies demonstrate that the Ki values of the cloned rat beta 3-AR and of the low affinity sites in IBAT are 45 and 29 nM, respectively, for BRL 37344 and 1.4 and 1.0 microM, for (-)-propranolol. These findings strongly suggest that the low affinity [3H]CGP 12177 binding site measured in IBAT plasma membranes represents the atypical beta 3-AR in this tissue.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adipose Tissue, Brown / metabolism*
  • Adrenergic beta-Antagonists / metabolism*
  • Animals
  • Binding, Competitive
  • CHO Cells
  • Cricetinae
  • Propanolamines / metabolism*
  • Radioligand Assay
  • Rats
  • Rats, Inbred Strains
  • Receptors, Adrenergic, beta / metabolism*
  • Tritium

Substances

  • Adrenergic beta-Antagonists
  • Propanolamines
  • Receptors, Adrenergic, beta
  • Tritium
  • CGP 12177