The cloning, sequencing and expression in model systems of the previou
sly unidentified beta(3)-adrenoceptor recently led to an extensive fun
ctional characterization. Ligand binding and adenylate cyclase activat
ion studies helped define a specific profile that is quite distinct fr
om that of the beta(1)- and beta(2)-adrenoceptors, but strongly remini
scent of most of the 'atypical' beta-adrenoceptor-mediated responses r
eported in earlier pharmacological studies. More recently, a naturally
occurring variation in the human beta(3)-adrenoceptor has been correl
ated with hereditary obesity and with increased dynamic capacity to ad
d on weight and develop non-insulin dependent diabetes in Western obes
e patients. Donny Strosberg and France Pietri-Rouxel describe how resu
lts now provide a consistent picture of an important role for the huma
n beta(3)-adrenoceptor in the regulation of lipid metabolism and as an
obvious target for drugs to treat some forms of obesity and diabetes.