Molecular characterization of the human beta 3-adrenergic receptor

Science. 1989 Sep 8;245(4922):1118-21. doi: 10.1126/science.2570461.


Since the classification of beta-adrenergic receptors (beta-ARs) into beta 1 and beta 2 subtypes, additional beta-ARs have been implicated in the control of various metabolic processes by catecholamines. A human gene has been isolated that encodes a third beta-AR, here referred to as the "beta 3-adrenergic receptor." Exposure of eukaryotic cells transfected with this gene to adrenaline or noradrenaline promotes the accumulation of adenosine 3',5'-monophosphate; only 2 of 11 classical beta-AR blockers efficiently inhibited this effect, whereas two others behaved as beta 3-AR agonists. The potency order of beta-AR agonists for the beta 3-AR correlates with their rank order for stimulating various metabolic processes in tissues where atypical adrenergic sites are thought to exist. In particular, novel beta-AR agonists having high thermogenic, antiobesity, and antidiabetic activities in animal models are among the most potent stimulators of the beta 3-AR.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic beta-Agonists / pharmacology
  • Adrenergic beta-Antagonists / pharmacology
  • Amino Acid Sequence
  • Animals
  • Cell Line
  • Cloning, Molecular
  • Cricetinae
  • Cyclic AMP / metabolism
  • Humans
  • Molecular Sequence Data
  • Receptors, Adrenergic, beta / drug effects
  • Receptors, Adrenergic, beta / genetics
  • Receptors, Adrenergic, beta / isolation & purification*
  • Sequence Homology, Nucleic Acid
  • Transfection


  • Adrenergic beta-Agonists
  • Adrenergic beta-Antagonists
  • Receptors, Adrenergic, beta
  • Cyclic AMP

Associated data

  • GENBANK/M29932