کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1377558 | 981981 | 2007 | 6 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Discovery of potent and orally bioavailable heterocycle-based β3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity Discovery of potent and orally bioavailable heterocycle-based β3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity](/preview/png/1377558.png)
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.
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. Compound 17 showed excellent agonist potency at the β3-AR, and a favorable pharmacokinetic profile in vivo. This compound increased rat oxygen consumption after oral administration, with an ED20% of 2 mg/kg.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 18, 15 September 2007, Pages 5245–5250