Tavapadon
产品说明书
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同义名 : | PF-06649751; CVL-751; PF-6649751 |
| CAS号 : | 1643489-24-0 | |
| 货号 : | A1380175 | |
| 分子式 : | C19H16F3N3O3 | |
| 纯度 : | 97% | |
| 分子量 : | 391.34 | |
| MDL号 : | MFCD32669809 | |
| 存储条件： |
Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Tavapadon is an orally active and highly selective dopamine D1/D5 receptor partial agonist. It may be useful in the treatment of Parkinson's disease and Alzheimer's. Tavapadon (0.1 mg/kg, s.c.) has the mean maximal unbound plasma concentration of 8 nM and achieves 3 hours after compound administration in captive-bred macaques. Tavapadon (0.02 and 0.04 mg/kg, s.c.) at the 0.04 mg/kg test dose increases locomotor activity, whereas the 0.02 mg/kg dose has little or no effect. Tavapadon (0.04 mg/kg, s.c.) also improves parkinsonian disability scores with the maximal improvement observed at 110 min after drug administration. Higher doses of Tavapadon (0.1 and 0.15 mg/kg, s.c.) cause statistically significant improvement relative to vehicle in locomotor activity[1]. The most frequently reported adverse events in patients treated with tavapadon were nausea, headache, dry mouth, somnolence, and tremor[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.56mL 0.51mL 0.26mL |
12.78mL 2.56mL 1.28mL |
25.55mL 5.11mL 2.56mL |
| 参考文献 |
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