Effects of several putative beta 3-adrenoceptor agonists on lipolysis in human omental adipocytes

Int J Obes Relat Metab Disord. 1996 May;20(5):428-34.


Background: Atypical beta 3-adrenoceptor agonists have attained an increasing interest as potential drugs against obesity and diabetes. However, their pharmacological actions on the native, human beta 3-adrenoceptor are not well defined.

Design: In the present study, the lipolytic effects of several putative beta 3-adrenoceptor agonists were investigated in human omental adipocytes.

Results: CL 316 243 and CGP 12177 had selective partial beta 3-agonist effects (pD2 about 4 and 8, respectively); the latter drug is a beta 1-/beta 2-adrenoceptor blocker in addition to its beta 3-adrenoceptor agonist activity. BRL 37344 and SM 11044 were also partial agonists, but with significant beta 1- and/or beta 2-adrenoceptor agonist properties. Bucindolol, ZD 2079, ICI D7114 and SR 58611A were ineffective as lipolytic drugs. In addition, ICI D7114 was a non-selective beta 1-/beta 2-/beta 3-adrenoceptor antagonist in human adipocytes.

Conclusion: None of the beta 3-adrenoceptor agonists tested is an ideal drug for therapeutic use in man (i.e. regarded as a selective and full agonist with high receptor potency). Only CL 316 243 may have a potential therapeutic role, although the potency is very low. CGP 12177 is useful as a reference substance for human in vitro studies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adipocytes / drug effects
  • Adipocytes / metabolism*
  • Adrenergic beta-Agonists / pharmacology*
  • Catechols / pharmacology
  • Dioxoles / pharmacology
  • Ethanolamines / pharmacology
  • Glycerol / metabolism
  • Humans
  • Isoproterenol / pharmacology
  • Lipolysis / drug effects*
  • Omentum*
  • Propanolamines / pharmacology
  • Serine / analogs & derivatives
  • Serine / pharmacology


  • Adrenergic beta-Agonists
  • Catechols
  • Dioxoles
  • Ethanolamines
  • Propanolamines
  • disodium (R,R)-5-(2-((2-(3-chlorophenyl)-2-hydroxyethyl)-amino)propyl)-1,3-benzodioxole-2,3-dicarboxylate
  • SM 11044
  • Serine
  • BRL 37344
  • Isoproterenol
  • Glycerol
  • CGP 12177