期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 3, 期 8, 页码 637-639出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml3000676
关键词
lactate receptor; GPR81; HCA1; nicotinic acid receptor; GPR109a; agonist; lipolysis; flushing; FFA
Following the characterization of the lactate receptor (GPR81), a focused screening effort afforded 3-hydroxybenzoic acid 1 as a weak agonist of both GPR81 and GPR109a (niacin receptor). An examination of structurally similar arylhydroxy acids led to the identification of 3-chloro-5-hydroxybenzoic acid 2, a selective GPR81 agonist that exhibited favorable in vivo effects on lipolysis in a mouse model of obesity.
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