g protein-coupled receptor 139

TAK-041 (NBI-1065846) 是一种选择性 GPR139激动剂，EC50为 22 nM，有用于精神分裂症阴性症状的研究潜力。

JNJ-63533054 是一种选择性的，具有口服活性的GPR139激动剂，对人GPR139的EC50为 16 nM。它可穿过血脑屏障，对 GPR139 的选择性高于其他 GPCR、离子通道和转运蛋白。

Selective medium-chain free fatty acid receptor GPR84 agonist (EC50 = 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 μM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1 2 phosphorylation, receptor desensitization and internalization in vitro. Liu et al (2016) Design and synthesis of 2-alkylpyrimidine-4,6-diol and 6-alkylpyridine-2,4-diol as potent GPR84 agonists. ACS Med.Chem.Lett. 7 579 PMID:27326330 |Zhang et al (2016) Discovery and characterization of a novel small-molecule agonist for medium-chain free fatty acid receptor G protein-coupled receptor 84. J.Pharmacol.Exp.Ther. 357 337 PMID:26962172