SYN115（Tozadenant）是一种新型的，具有口服活性的，选择性的腺苷受体A2aR拮抗剂，能改善帕金森病动物模型的运动功能。
别名：Tozadenant
SYN115（Tozadenant）是一种新型的，具有口服活性的，选择性的腺苷受体A2aR拮抗剂，能改善帕金森病动物模型的运动功能。
| 体外实验* | |
|---|---|
| 细胞系 | CHO cells |
| 方法 | A1 and A2B adenosine receptor functional assay CHO cells, expressing recombinant human ARs, were harvested by trypsinization. After centrifugation and re-suspension in medium, cells (~30,000) were plated in 24-well plates in 0.5 mL of medium. After 24 h, the medium was removed, and the cells were incubated at 37℃ for 15 min with 0.5 mL of Dulbecco's Modified Eagle Medium (DMEM) in the presence of adenosine deaminase (ADA) (1 U/mL) and the phosphodiesterase inhibitor Ro20-1724 (20 mM). The pharmacological profile of the compounds towards A2B ARs was evaluated by assessing cAMP accumulation in the absence or presence of the agonist NECA (100 nM). The antagonist profile of the compounds towards A1 ARs was evaluated by assessing their ability to counteract NECA-mediated inhibition of cAMP accumulation in the presence of 1 mM forskolin, as non-selective adenylate cyclase (AC) activator. Cells were incubated in the reaction medium (15 min at 37℃) with different concentrations of target compounds (0.1 nM~1 mM) and then were treated with the agonist. Following incubation, the reaction was terminated by the removal of the medium and the addition of 0.4 N HCl. After 30 min, lysates were neutralized with 4 N KOH, and the suspension was centrifuged at 800 g for 5 min. For the determination of cAMP production, bovine adrenal cAMP binding protein was incubated with [3H]cAMP (2 nM) and 50 ml of cell lysate or cAMP standard (0~160 pmol) at 0℃for 150 min in a total volume of 300 ml. Bound radioactivity was separated by rapid filtration through GF/C glass fiber filters and washed twice with 4 mL 50 mM TriseHCl, pH 7.4. The radioactivity was measured by liquid scintillation spectrometry. |
| 浓度 | 0~1μM |
| 处理时间 | 15 min |
*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。
| 体内实验* | |
|---|---|
| 动物模型 | male Swiss albino mice(23~25 g) |
| 配制 | isotonic (NaCl 0.9%) saline solution |
| 剂量 | 3, 10 and 30mg/kg was given immediately after punishment |
| 给药处理 | i.p. |
*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。
| 分子量 | 406.5 |
| 分子式 | C19H26N4O4S |
| CAS号 | 870070-55-6 |
| 溶解性（25°C） | DMSO 10 mM |
| 储存条件 |
粉末型式 -20°C 3年；4°C 2年 溶于溶剂 -80°C 6个月；-20°C 1个月 |
| 运输方式 | 冰袋运输，根据产品的不同，可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.46 mL | 12.3001 mL | 24.6002 mL |
| 5 mM | 0.492 mL | 2.46 mL | 4.92 mL |
| 10 mM | 0.246 mL | 1.23 mL | 2.46 mL |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
| 其他相关的Adenosine Receptor产品 |
|---|
| LUF5519
LUF5519 is a ribose-containing adenosine A1 receptor agonist. |
| LUF6258
LUF6258 is a hybrid ortho/allosteric ligand of the adenosine A(1) receptor. |
| A3AR agonist 1
A3AR agonist 1 是一种 A3AR 激动剂 (Ki: 25.8 nM)。 |
| A3AR agonist 2
A3AR agonist 2 是一种选择性的 A3AR 激动剂 (Ki: 22.1 nM)。 |
| Inupadenant hydrochloride
Inupadenant (EOS-850) hydrochloride 是一种具有口服活性的，高选择性 A2A 受体拮抗剂。 |
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