A cloned human beta (3) adrenergic receptor assay was used to identify pote
nt and selective beta (3) agonists. The thiazolidinedione moiety has been i
dentified as a new pharmacophore for the human beta (3) adrenergic receptor
. The versatility of the thiazolidinedione pharmacophore was demonstrated i
n both the arylethanolamine and phenylpropanolamine families of beta (3) ag
onists, where potent and selective compounds have been synthesized. Thiazol
idinedione 20, a potent and selective human beta (3) agonist, increased the
rmogenesis and lowered plasma glucose levels in the db/db mice.