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Science 8 September 1989:
Vol. 245. no. 4922, pp. 1118 - 1121
DOI: 10.1126/science.2570461

Articles

Science, Vol 245, Issue 4922, 1118-1121
Copyright © 1989 by American Association for the Advancement of Science


articles

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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In Vivo Increase in {beta}-Adrenergic Lipolytic Response in Subcutaneous Adipose Tissue of Obese Subjects Submitted to a Hypocaloric Diet.
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J. Cell Sci. 107, 313-319
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beta 3- and alpha 1-Adrenergic Erk1/2 Activation Is Src- but Not Gi-mediated in Brown Adipocytes.
J. M. Lindquist, J. M. Fredriksson, S. Rehnmark, B. Cannon, and J. Nedergaard (2000)
J. Biol. Chem. 275, 22670-22677
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Upregulation of Functional {beta}3-Adrenergic Receptor in the Failing Canine Myocardium.
H.-J. Cheng, Z.-S. Zhang, K. Onishi, T. Ukai, D. C. Sane, and C.-P. Cheng (2001)
Circ. Res. 89, 599-606
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