Title of article
Discovery of potent and orally bioavailable heterocycle-based β3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
6
From page
5245
To page
5250
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.
Keywords
obesity , ?3-Adrenergic receptor agonists , thermogenesis
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798591
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