| Literature DB >> 16102966 |
Dong-Ming Shen1, Fengqi Zhang, Edward J Brady, Mari Rios Candelore, Qing Dallas-Yang, Victor D-H Ding, Jasminka Dragovic, William P Feeney, Guoquiang Jiang, Peggy E McCann, Steve Mock, Sajjad A Qureshi, Richard Saperstein, Xiaolan Shen, Constantin Tamvakopoulos, Xinchun Tong, Laurie M Tota, Michael J Wright, Xiaodong Yang, Song Zheng, Kevin T Chapman, Bei B Zhang, James R Tata, Emma R Parmee.
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.Entities:
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Year: 2005 PMID： 16102966 DOI： 10.1016/j.bmcl.2005.06.101
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823