Author/Authors :
Jennifer A. Lafontaine، نويسنده , , Robert F. Day، نويسنده , , Joe Dibrino، نويسنده , , John R. Hadcock، نويسنده , , Diane M. Hargrove، نويسنده , , Michael Linhares، نويسنده , , Kelly A. Martin، نويسنده , , Tristan S. Maurer، نويسنده , , Nancy A. Nardone، نويسنده , , David A. Tess، نويسنده , , Paul DaSilva-Jardine، نويسنده ,
Abstract :
A novel series of heterocycle-based analogs were prepared and evaluated for their in vitro and in vivo biological activity as human β3-adrenergic receptor (AR) agonists. Several analogs demonstrated potent agonist activity at the β3-AR, functional selectivity against β1- and β2-ARs, and favorable pharmacokinetic profiles in vivo. Compound 17 increased oxygen consumption in rats, a measure of energy expenditure, with an ED20% of 2 mg/kg.
