- The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators.
The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators.
Bioorganic & medicinal chemistry letters (2009-12-17)
Yingcai Wang, Xianyun Jiao, Frank Kayser, Jiwen Liu, Zhongyu Wang, Malgorzata Wanska, Joanne Greenberg, Jennifer Weiszmann, Hongfei Ge, Hui Tian, Simon Wong, Ralf Schwandner, Taeweon Lee, Yang Li
PMID20005104
摘要
Free fatty acid receptor 2 (FFA2) is a G-protein coupled receptor for which only short-chain fatty acids (SCFAs) have been reported as endogenous ligands. We describe the discovery and optimization of phenylacetamides as allosteric agonists of FFA2. These novel ligands can suppress adipocyte lipolysis in vitro and reduce plasma FFA levels in vivo, suggesting that these allosteric modulators can serve as pharmacological tools for exploring the potential function of FFA2 in various disease conditions.
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乙酸, glacial, puriss., meets analytical specification of Ph. Eur., BP, USP, 99.8-100.5%