173901-05-8Relevant articles and documents
Potent, selective aminothiazolidinediones agonists of the human β3 Adrenergic receptor
Malamas,Largis,Gunawan,Li,Tillett,Han,Mulvey
, p. 164 - 177 (2007/10/03)
A cloned human β3 adrenergic receptor assay was used to identify potent and selective β3 agonists. The thiazolidinedione moiety has been identified as a new pharmacophore for the human β3 adrenergic receptor. The versatility of the thiazolidinedione pharmacophore was demonstrated in both the arylethanolamine and phenylpropanolamine families of β3 agonists, where potent and selective compounds have been synthesized. Thiazolidinedione 20, a potent and selective human β3 agonist, increased thermogenesis and lowered plasma glucose levels in the db/db mice.
3-pyridylethanolamines: Potent and selective human β3 adrenergic receptor agonists
Naylor, Elizabeth M.,Colandrea, Vincent J.,Candelore, Mari R.,Cascieri, Margaret A.,Colwell Jr., Lawrence F.,Deng, Liping,Feeney, William P.,Forrest, Michael J.,Hom, Gary J.,MacIntyre, D. Euan,Strader, Catherine D.,Tota, Laurie,Wang, Pei-Ran,Wyvratt, Matthew J.,Fisher, Michael H.,Weber, Ann E.
, p. 3087 - 3092 (2007/10/03)
The 3-pyridylethanolamine L-757,793 is a potent β3 AR agonist (EC50 6.3 nM, 70% activation) with 1,300- and 500-fold selectivity over binding to the β1 and β2 ARs, respectively. L-757,793 stimulated lipolysis in rhesus monkeys (ED50 0.2 mg/kg) with a maximum response equivalent to that elicited by isoproterenol.
