| 名称 | Aticaprant |
| 描述 | Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).[2] |
| 动物实验 | 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]. |
| 体外活性 | Aticaprant(CERC-501) binds with a high affinity to the human kappa opioid receptor with a 30-fold higher affinity over the human mu-opioid receptor and a 190-fold higher affinity over the human delta-opioid receptor. Aticaprant(CERC-501) shows no appreciable affinity for several non-opioid cell surface G-protein-coupled receptor targets [1]. |
| 体内活性 | METHODS: Mice were given Aticaprant(CERC-501) (0.1 to 3 mg/kg, intraperitoneal injection) 30 minutes before the alcohol deprivation effect (ADE) test and naltrexone (0.3 or 1 mg/kg, intraperitoneal injection) 10 minutes before the test to observe the effect of aticaprant on the ADE effect.
RESULTS 0.3 mg/kg of Aticaprant(CERC-501) and 1 mg/kg of naltrexone reduced the ADE alcohol intake of mice at 4 hours. [1] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 100 mg/mL (238.95 mM)
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| 关键字 | inhibit | Opioid Receptor | CERC501 | Inhibitor | CERC 501 | Aticaprant | LY2456302 | LY 2456302 |
| 相关产品 | Docusate sodium | Bevenopran | Mirtazapine | Sinomenine | (-)-Menthol | Matrine | SCH 221510 | Progesterone | Naltrexone hydrochloride | Trimebutine | Mianserin hydrochloride | Amentoflavone |
| 相关库 | 经典已知活性库 | 疼痛相关化合物库 | 神经退行性疾病化合物库 | 膜蛋白靶向化合物库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抑制剂库 | 已知活性化合物库 | GPCR靶点分子库 | 抗癌药物库 |
United States
