2-PCCAhydrochloride是一种外消旋体，为GPR88受体激动剂，在HEK293细胞中，可抑制GPR88介导的cAMP的产生，EC50值为116nM。
货号:ajcx13472
CAS:N/A
分子式:C60H76Cl2N6O2
分子量：984.19
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

2-PCCA hydrochloride is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.

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].

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].

[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.

Protocol:

Animal experiment:

Rats[1]For the locomotor activity tests, rats are only used once. The test is conducted in an adjacent room from the animal colony room with similar environmental conditions (light, temperature and humidity). Before tests begin, rats are exposed to at least three days of handling by the experimenter. When only 2-PCCA (1.0 and 3.2 mg/kg) is studied, the drug is (i.p.) injected immediately before the rats are put into the test chambers and the locomotor activity is simultaneously recorded for 60 min. When 2-PCCA is studied in combination with methamphetamine, the locomotor activity is recorded for 20 min and then both drugs are simultaneously injected and the locomotor activity is recorded for 120 more min[1].

参考文献: [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.