2-PCCA (hydrochloride)

2-PCCA hydrochloride is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC₅₀ of 116 nM in HEK293 cells. IC50 & Target: EC50: 116 nM (GPR88 receptor, HEK293 cells)^[1] In Vitro: 2-PCCA hydrochloride inhibits GPR88-mediated cAMP production through a Gαi-coupled pathway, with an EC₅₀ of 116 nM in HEK293 cells stably expressing the human GPR88 receptor and the GloSensor-22F cAMP construct^[2]. In Vivo: 2-PCCA (0.1-3.2 mg/kg, i.p.) decreases the locomotor activity in rats in a dose-dependent manner in rats. 2-PCCA combined with 1.0 mg/kg methamphetamine also dose-dependently reduces methamphetamine-induced hyperactivity. 2-PCCA (1-3.2 mg/kg, i.p.) alone does not produce methamphetamine-like discriminative stimulus effects, or alter the discriminative stimulus effects of methamphetamine, when studied in combination^[1].