Abstract
Brown adipose tissue dissipates energy in the form of heat via uncoupling protein (UCP)-1 and has attracted much attention as a therapeutic target for the treatment of obesity and related diseases such as type 2 diabetes. Lipolysis and thermogenesis in white and brown adipocytes are stimulated by the sympathetic nervous system through the adrenergic receptors on the plasma membrane. The β3-adrenergic receptor agonist is an excellent candidate for the treatment of obesity because the β3 isoform is expressed exclusively in adipocytes and is therefore devoid of actions on other cell types such as cardiomyocytes and smooth muscle cells through the other isoforms-β1 and β2. The attempts to develop clinically useful β3-adrenergic receptor agonists, however, have failed because of inadequate bioavailability and efficacy in humans1 .
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