Selective medium-chain free fatty acid receptor GPR84 agonist (EC50
= 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 uM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1/2 phosphorylation, receptor desensitization and internalization in vitro
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Design and synthesis of 2-alkylpyrimidine-4,6-diol and 6-alkylpyridine-2,4-diol as potent GPR84 agonists.
Liu et al.
ACS Med.Chem.Lett., 2016;7:579
Discovery and characterization of a novel small-molecule agonist for medium-chain free fatty acid receptor G protein-coupled receptor 84.
Zhang et al.