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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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4025785 | PMC |
| http://dx.doi.org/10.1021/ml3000676 | DOI Listing |
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