[Adenylate cyclase response to beta-adrenergic agonists in heart and brown adipose tissue]

Minerva Endocrinol. 1990 Apr-Jun;15(2):125-9.
[Article in Italian]

Abstract

Some sympathomimetic compounds (i.e. BRL37344) increase brown adipose tissue (BAT) thermogenesis with minimal cardiac effects. They act through an "atypical" beta-adrenergic receptor (beta-AR). Since beta-AR responses involve Adenylate Cyclase (AC) activation, we investigate the AC answer to isoproterenol and BRL37344 in rat plasmamembranes of heart (beta 1-ARs) and BAT (atypical beta-ARs). AC dose-response curves were obtained by incubating membrane fractions with different concentrations of isoproterenol and BRL37344 (1 nM-100 microM) at 25 degrees C for 15 min. In our study BRL37344 is 40-times more potent than isoproterenol in stimulating AC activity of BAT (EC50s: BRL37344 = 0.02 microM, isoproterenol = 0.7 microM). Furthermore it is more potent in stimulating BAT AC than heart AC (BRL37344 EC50 ratio heart/BAT = 38). However on BAT membranes, BRL37344 intrinsic sympathomimetic activity (ISA) vs. Isoproterenol is 0.87. Since isoproterenol and BRL37344 show a similar ISA for BAT respiration and lipolysis, we may argue that AC maximal activity is not required for maximal lipolytic and thermogenic responses.

MeSH terms

  • Adenylyl Cyclases / metabolism*
  • Adipose Tissue / drug effects
  • Adipose Tissue / enzymology*
  • Adrenergic beta-Agonists / pharmacology*
  • Animals
  • Dose-Response Relationship, Drug
  • Ethanolamines / pharmacology
  • Heart / drug effects
  • Isoproterenol / pharmacology
  • Male
  • Myocardium / enzymology*
  • Rats
  • Rats, Inbred Strains

Substances

  • Adrenergic beta-Agonists
  • Ethanolamines
  • BRL 37344
  • Adenylyl Cyclases
  • Isoproterenol