| Literature DB >> 18539028 |
Ronald M Kim1, Jiang Chang, Ashley R Lins, Ed Brady, Mari R Candelore, Qing Dallas-Yang, Victor Ding, Jasminka Dragovic, Susan Iliff, Guoqiang Jiang, Steven Mock, Sajjad Qureshi, Richard Saperstein, Deborah Szalkowski, Constantin Tamvakopoulos, Laurie Tota, Michael Wright, Xiaodong Yang, James R Tata, Kevin Chapman, Bei B Zhang, Emma R Parmee.
Abstract
The discovery and optimization of potent and selective aminobenzimidazole glucagon receptor antagonists are described. One compound possessing moderate pharmacokinetic properties in multiple preclinical species was orally efficacious at inhibiting glucagon-mediated glucose excursion in transgenic mice expressing the human glucagon receptor, and in rhesus monkeys. The compound also significantly lowered glucose levels in a murine model of diabetes.Entities:
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Year: 2008 PMID： 18539028 DOI： 10.1016/j.bmcl.2008.05.072
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823