1301211-78-8
1301211-78-8 结构式
物理化学性质
沸点480.0±45.0 °C(Predicted)
密度1.168±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO: 60 mg/mL (258.31 mM)
酸度系数(pKa)15.67±0.40(Predicted)
形态Solid
颜色Light yellow to yellow
常见问题列表
生物活性
E1R 是一种 sigma-1 受体的正变构调节剂 (Sig1R PAM)，具有认知增强效果。体外研究
The only target for E1R (inhibition or enhancement of radioligand binding exceeding 20%) is the sigma receptor. 10 μM E1R does not displace the radioligand, but instead increases the specific binding of a non-selective radioligand ([ 3 H]1,3-di(2-tolyl)guanidine) for the sigma receptor by 38% in Jurkat cells.
体内研究
E1R demonstrates efficacy against scopolamine-induced cholinergic dysfunction in mice. Treatment with E1R (0.1-10 mg/kg; administered i.p. 60 min before the training session) significantly improves cognitive function in a dose-related manner in mice.
| Animal Model: | Male ICR and Balb/c mice weighed 23-25 g |
| Dosage: | 0.1, 1 and 10 mg/kg |
| Administration: | Administered i.p. 60 min before the training session |
| Result: | Treatment at doses of 1 and 10 mg/kg increased retention latency by 194 and 211%, respectively, compared with the control group. |