| Literature DB >> 21147532 |
Dong-Ming Shen1, Edward J Brady, Mari R Candelore, Qing Dallas-Yang, Victor D-H Ding, William P Feeney, Guoquiang Jiang, Margaret E McCann, Steve Mock, Sajjad A Qureshi, Richard Saperstein, Xiaolan Shen, 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 1,3,5-pyrazoles has been discovered as potent human glucagon receptor antagonists. Notably, compound 26 is orally bioavailable in several preclinical species and shows selectivity towards cardiac ion channels, other family B receptors such hGIP and hGLP1, and a large panel of enzymes and additional receptors. When dosed orally, compound 26 is efficacious in suppressing glucagon induced plasma glucose excursion in rhesus monkey and transgenic murine pharmacodynamic models at 1 and 10 mpk, respectively.Entities:
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Year: 2010 PMID： 21147532 DOI： 10.1016/j.bmcl.2010.11.074
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823