化合物A-437203 T10213
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Product IntroductionBioactivity英文名: A-437203描述: A-437203 (Lu201640) 是一种基于1H-pyrimidin-2-one scaffold 的、具有选择性的、新型强效的d3受体拮抗剂
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Product Introduction
Bioactivity
英文名: A-437203
描述: A-437203 (Lu201640) 是一种基于1H-pyrimidin-2-one scaffold 的、具有选择性的、新型强效的d3受体拮抗剂，对 D2, D3, 和 D4 受体,的Ki 值分别为 71, 1.6 和 6220 nM。
动物实验: Male Sprague-Dawley rats weighing 250-350 g are used for these experiments. Haloperidol (0.27, 1.33, and 2.66 μmol/kg=0.1, 0.5, and 1.0 mg/kg i.p.), A-437203 (LU-201640) (0.52, 1.75, 5.24, and 17.46 μmol/kg=0.3, 1.0, 3.0, and 10.0 mg/kg i.p.), and L-745,870 (0.23, 1.15, 2.3, and 5.7 μmol/kg=0.1, 0.5, 1.0, and 2.5 mg/kg i.p.) are tested initially alone in order to determine effective dose ranges. In those experiments, haloperidol, A-437203, and L-745,870 are administered i.p. 24, 5, and 0.5 h before the test swim. In the subsequent antagonism experiments, Haloperidol (0.27 μmol/kg), A-437203 (17.46 μmol/kg) or L-745,870 (1.15 μmol/kg) are injected i.p. 15 min prior to each quinpirole injection (0.4 and 1.0 μmol/kg s.c.).
体外活性: A-437203是一种具有高亲和力的D3受体拮抗剂，并相对于其他多巴胺受体亚型具有较高的选择性（与D2相比，对D3的选择性高出44倍）[1]。
体内活性: A-437203在大鼠强迫游泳测试（FST）中单独测试。A-437203剂量为0.52、1.75、5.24和17.46 μmol/kg，注射方式为静脉注射。剂量的选择基于A-437203对D3与D2多巴胺受体的选择性。17.46 μmol/kg（10 mg/kg）或更低剂量的A-437203效果明显由D3受体介导，而非D2受体。174.6 μmol/kg（100 mg/kg）等高剂量的化合物才能结合并阻断D2受体，避免被烷化剂EEDG不可逆地失活。方差分析（ANOVA）表明，对于分析的任何行为，各处理组之间无显著差异（对于不动行为F4, 45=1.12, p=0.359，对于攀爬行为F4, 45=0.188, p=0.943，对于游泳行为F4, 45=1.634, p=0.182）。基于这些结果，选择17.46 μmol/kg静脉注射剂量的A-437203进行进一步实验[1]。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 60 mg/mL (131.43 mM)
关键字: A-437203 | A-37203 | ABT925 | ABT 925 | A 437203 | A437203 | A 37203
相关产品: Flibanserin | Centanafadine hydrochloride | 9-FLUORENOL | Blonanserin | ONC206 | L-741626 | GR 103691 | Methyldopa hydrate | Sultopride hydrochloride | Brexpiprazole
相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | GPCR Compound Library | Bioactive Compound Library
Bioactivity
英文名: A-437203
描述: A-437203 (Lu201640) 是一种基于1H-pyrimidin-2-one scaffold 的、具有选择性的、新型强效的d3受体拮抗剂，对 D2, D3, 和 D4 受体,的Ki 值分别为 71, 1.6 和 6220 nM。
动物实验: Male Sprague-Dawley rats weighing 250-350 g are used for these experiments. Haloperidol (0.27, 1.33, and 2.66 μmol/kg=0.1, 0.5, and 1.0 mg/kg i.p.), A-437203 (LU-201640) (0.52, 1.75, 5.24, and 17.46 μmol/kg=0.3, 1.0, 3.0, and 10.0 mg/kg i.p.), and L-745,870 (0.23, 1.15, 2.3, and 5.7 μmol/kg=0.1, 0.5, 1.0, and 2.5 mg/kg i.p.) are tested initially alone in order to determine effective dose ranges. In those experiments, haloperidol, A-437203, and L-745,870 are administered i.p. 24, 5, and 0.5 h before the test swim. In the subsequent antagonism experiments, Haloperidol (0.27 μmol/kg), A-437203 (17.46 μmol/kg) or L-745,870 (1.15 μmol/kg) are injected i.p. 15 min prior to each quinpirole injection (0.4 and 1.0 μmol/kg s.c.).
体外活性: A-437203是一种具有高亲和力的D3受体拮抗剂，并相对于其他多巴胺受体亚型具有较高的选择性（与D2相比，对D3的选择性高出44倍）[1]。
体内活性: A-437203在大鼠强迫游泳测试（FST）中单独测试。A-437203剂量为0.52、1.75、5.24和17.46 μmol/kg，注射方式为静脉注射。剂量的选择基于A-437203对D3与D2多巴胺受体的选择性。17.46 μmol/kg（10 mg/kg）或更低剂量的A-437203效果明显由D3受体介导，而非D2受体。174.6 μmol/kg（100 mg/kg）等高剂量的化合物才能结合并阻断D2受体，避免被烷化剂EEDG不可逆地失活。方差分析（ANOVA）表明，对于分析的任何行为，各处理组之间无显著差异（对于不动行为F4, 45=1.12, p=0.359，对于攀爬行为F4, 45=0.188, p=0.943，对于游泳行为F4, 45=1.634, p=0.182）。基于这些结果，选择17.46 μmol/kg静脉注射剂量的A-437203进行进一步实验[1]。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 60 mg/mL (131.43 mM)
关键字: A-437203 | A-37203 | ABT925 | ABT 925 | A 437203 | A437203 | A 37203
相关产品: Flibanserin | Centanafadine hydrochloride | 9-FLUORENOL | Blonanserin | ONC206 | L-741626 | GR 103691 | Methyldopa hydrate | Sultopride hydrochloride | Brexpiprazole
相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | GPCR Compound Library | Bioactive Compound Library
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