PMID: 11311069Apr 20, 2001Paper

(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists

Journal of Medicinal Chemistry
B HuJ Tillett

Abstract

In search of potent and selective human beta(3) agonists as potential drugs for the treatment of human obesity and type II diabetes, a series of (4-piperidin-1-yl)phenyl amides was prepared and evaluated for their biological activity on the human beta(3)-adrenergic receptor. The leucine derivative 26e and the reverse amide 33b were found to be the two most potent and selective compounds in this study. With EC(50) values of 0.008 and 0.009 microM, respectively, at the beta(3) receptor, nearly completely abolished intrinsic activity at either the beta(1) or beta(2) receptor, and significant thermogenesis effects on human beta(3)-adrenergic receptor transgenic mice, 26e and33b are among the most potent and selective human beta(3) agonists known to date.

References

Nov 1, 1987·Proceedings of the National Academy of Sciences of the United States of America·T FrielleB K Kobilka
Dec 8, 1995·The Journal of Biological Chemistry·V S SusulicB B Lowell

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Citations

Dec 21, 2010·Medicinal Chemistry Research : an International Journal for Rapid Communications on Design and Mechanisms of Action of Biologically Active Agents·P Senthil Kumar, Prasad V Bharatam
May 30, 2007·Bioorganic & Medicinal Chemistry Letters·W N WashburnP M Sher
Aug 3, 2005·Journal of Computer-aided Molecular Design·Philip Prathipati, Anil K Saxena
Mar 18, 2011·Expert Opinion on Therapeutic Patents·Maria Grazia Perrone, Antonio Scilimati

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