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Science 8 September 1989: Vol. 245. no. 4922, pp. 1118 - 1121 DOI: 10.1126/science.2570461
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Articles
Science, Vol 245, Issue 4922, 1118-1121
Copyright © 1989 by American Association for the Advancement of Science
Molecular characterization of the human beta 3-adrenergic receptor
LJ Emorine,
S Marullo,
MM Briend-Sutren,
G Patey,
K Tate,
C Delavier-Klutchko,
and
AD Strosberg
CNRS, Universite Paris VII, France.
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.
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