MOLECULAR CHARACTERIZATION OF THE HUMAN BETA-3-ADRENERGIC RECEPTOR
MOLECULAR CHARACTERIZATION OF THE HUMAN BETA-3-ADRENERGIC RECEPTOR
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DOI：
10.1126/science.2570461
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发表时间：
1989-09-08
期刊：
影响因子：
56.9
通讯作者：
STROSBERG, AD
中科院分区：
文献类型：
--
作者：
EMORINE, LJ;MARULLO, S;STROSBERG, AD
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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 potent stimulators of the .beta.3-AR.