生物活性
8-OH-DPAT (8-Hydroxy-DPAT)是一种有效的选择性5-HT1A激动剂，pIC50为8.19。8-OH-DPAT在5-HT7上具有高亲和力，Ki为466 nM。
在体内研究中，8-OH-DPAT（1 mg/kg）显著增加觉醒并减少REM睡眠的持续时间，而不影响orexin敲除（KO）小鼠黑暗期间非REM睡眠的持续时间。8-OH-DPAT是亲脂性分子，能够穿透血脑屏障。
化学数据
| 分子量 | 247.38 |
| 分子式 | C16H25NO |
| CAS号 | 78950-78-4 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO: ≥ 45 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | Retinal pigment epithelial (RPE) cells |
| 方法 | Cells are exposed to H2O2 (200 μM) for 1 hour and either pre-or post treated with 8-OH DPAT (10 μM) for 24 hours. In the case of pretreatment all measurements are made 24 hr after H2O2 and for post treatment 8-OH DPAT is added immediately following H2O2 exposure. 5HT1A agonist treatment: To assess the ability of the 5-HT1A receptor agonist, 8-OH DPAT, to reduce lipofuscin formation in cultured RPE cells, this compound is added to the culture medium every 48 hours at concentrations ranging from 0.1 to 20 μM. All experiments are undertaken in basal medium, and cells receiving vehicle alone (PBS) acted as negative controls. To determine if the effect of 8-OH DPAT is sustained following discontinuation of 5-HT1A receptor agonist treatment, 8-OH DPAT treatment is discontinued after 28 days and the cells maintained in basal medium or fed POS for a further 28 days. To assess the ability of 8-OH DPAT to remove existing lipofuscin, autophagy-derived lipofuscin and phagocytic-derived lipofuscin are allowed to accumulate as described above and then 8-OH DPAT is added every second day for up to 28 days. |
| 浓度 | 10 μM |
| 处理时间 | 24 h |
| 动物实验 |
|---|
| 动物模型 | Male Lister hooded rats |
| 配制 | isotonic saline |
| 剂量 | 0, 3.0, 10, 100 and 300 μg/kg |
| 给药处理 | i.p. |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 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。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.0424 mL | 20.2118 mL | 40.4236 mL |
| 5 mM | 0.8085 mL | 4.0424 mL | 8.0847 mL |
| 10 mM | 0.4042 mL | 2.0212 mL | 4.0424 mL |
m.cnreagent.com