| Bioactivity | 2-PCCA hydrochloride is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells. |
| Target | EC50: 116 nM (GPR88 receptor, HEK293 cells) |
| Invitro | 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]. |
| Name | 2-PCCA hydrochloride |
| Formula | C30H38ClN3O |
| Molar Mass | 492.10 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Li JX, et al. The GPR88 receptor agonist 2-PCCA does not alter the behavioral effects of methamphetamine in rats. Eur J Pharmacol. 2013 Jan 5;698(1-3):272-7. [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. |