Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).[2]

κ opioid:0.807 nM (Ki)

Aticaprant(CERC-501)与人类 κ 阿片受体的结合亲和力很高，比人类 μ 阿片受体的亲和力高 30 倍，比人类 delta 阿片受体的亲和力高 190 倍。Aticaprant(CERC-501)对几种非阿片细胞表面 G 蛋白偶联受体靶标没有明显的亲和力 [1]。

方法：在小鼠酒精剥夺效应（ADE）测试前30分钟接受aticaprant（0.1至3mg / kg，腹腔注射），测试前10分钟接受纳曲酮（0.3或1mg / kg，腹腔注射），观察aticaprant对ADE效应的影响。
结果：0.3 mg/kg 的 aticaprant 和 1 mg/kg 的纳曲酮，4 小时时小鼠ADE 酒精摄入量减少。[1]

Three male cannulated rats are administered a single 1 mg/kg intravenous (IV) and 10 mg/kg oral (PO) dose of Aticaprant to determine the pharmacokinetic parameters. Plasma samples are collected at 0.08 (IV only), 0.25, 0.5, 1, 2, 4, 8, 12 and 24 h post-dose and analyzed by liquid chromatography coupled to tandem mass spectral detection to determine the concentrations of Aticaprant (CERC-501). Male mice are administered a single 10 mg/kg PO dose of Aticaprant to determine the pharmacokinetic parameters. Plasma samples are collected at 0.5, 1, 2, 4, 8, and 24 h post-dose and analyzed by LCMS/MS to determine the concentrations of Aticaprant. The plasma and brain binding of Aticaprant is determined by equilibrium dialysis at 1 μM [1].