Title of article
Discovery of novel, potent, and orally active spiro-urea human glucagon receptor antagonists
Author/Authors
Dong-Ming Shen، نويسنده , , Fengqi Zhang، نويسنده , , Edward J. Brady، نويسنده , , Mari Rios Candelore، نويسنده , , Qing Dallas-Yang، نويسنده , , Victor D.-H. Ding، نويسنده , , Jasminka Dragovic، نويسنده , , William P. Feeney، نويسنده , , Guoquiang Jiang، نويسنده , , Peggy E. McCann، نويسنده , , Steve Mock، نويسنده , , Sajjad A. Qureshi، نويسنده , , Richard Saperstein، نويسنده , , Xiaolan Shen، نويسنده , , Constantin Tamvakopoulos، نويسنده , , Xinchun Tong، نويسنده , , Laurie M. Tota، نويسنده , , Michael J. Wright، نويسنده , , Xiaoyan Ye and Xiaodong Yang، نويسنده , , Song Zheng، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
6
From page
4564
To page
4569
Abstract
A novel class of spiro-ureas has been discovered as potent human glucagon receptor antagonists in both binding and functional assays. Preliminary studies have revealed that compound 15 is an orally active human glucagon receptor antagonist in a transgenic murine pharmacodynamic model at 10 and 30 mpk. Compound 15 is orally bioavailable in several preclinical species and shows selectivity toward cardiac ion channels and other family B receptors, such as hGIP1 and hGLP.
Keywords
Glucagon receptor antagonists
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796034
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