2-PCCA hydrochloride is a potent, selective agonist of the orphan GPR88 receptor with EC50 of 877 nM. 2-PCCA inhibits isoproterenol-stimulated cAMP accumulation in a concentration-dependent manner in cells expressing GPR88 through a Gαi-coupled pathway. 2-PCCA dose-dependently decreases the locomotor activity in rats at 0.1-3.2mg/kg, also decreases methamphetamine-induced hyperactivity combined with methamphetamine. 2-PCCA does not alter the behavioral effects of methamphetamine in rats alone.
