LP-471756 is a potent GPR139 antagonist with an IC50 value of 640 nM. LP-471756 inhibits LP-360924-stimulated cAMP production[1][2].
LP-471756 (0-1000 µM) 特异性抑制 GPR139 细胞中 LP-360924 刺激的 cAMP 的生成,IC50 值为 0.64 µM[2]。
[1]. Vedel L, et al. Pharmacology and function of the orphan GPR139 G protein-coupled receptor. Basic Clin Pharmacol Toxicol. 2020 Jun;126 Suppl 6(Suppl 6):35-46.
[2]. Hu LA, et al. Identification of surrogate agonists and antagonists for orphan G-protein-coupled receptor GPR139. J Biomol Screen. 2009 Aug;14(7):789-97.
















