Tavapadon

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 activity¹. The most frequently reported adverse events in patients treated with tavapadon were nausea, headache, dry mouth, somnolence, and tremor².

溶解方案(细胞实验)

DMSO 中的溶解度 : 66.67 mg/mL (170.36 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: 2.5 mg/mL (6.39 mM); 澄清溶液; 超声助溶 此方案可获得 2.5 mg/mL的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"