(1R,2R)-2-PCCA(hydrochloride)

(1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and acts as a potent GPR88 receptor agonist, with an EC50 of 3 nM.

Signaling Pathways >> Others >> Others

Research Areas >> Neurological Disease

EC50: 3 nM (GPR88 receptor)[1]

(1R,2R)-2-PCCA hydrochloride is a potent GPR88 receptor agonist, with an EC50 of 3 nM[1]. (1R,2R)-2-PCCA inhibits GPR88-mediated cAMP production through a Gαi-coupled pathway, with an EC50 of 56 nM in HEK293 cells stably expressing the human GPR88 receptor and the GloSensor-22F cAMP construct[2].

[1]. Bi, Yingzhi, et al. Modulators of G Protein-Coupled Receptor 88. US 20110251204 A1.

[2]. Jin C, et al. Effect of Substitution on the Aniline Moiety of the GPR88 Agonist 2-PCCA: Synthesis, Structure-Activity Relationships, and Molecular Modeling Studies. ACS Chem Neurosci. 2016 Oct 19;7(10):1418-1432.

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