1301211-78-8
1301211-78-8 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
沸點(diǎn)480.0±45.0 °C(Predicted)
密度1.168±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 60 mg/mL (258.31 mM)
酸度系數(shù)(pKa)15.67±0.40(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
常見(jiàn)問(wèn)題列表
生物活性
E1R 是一種 sigma-1 受體的正變構(gòu)調(diào)節(jié)劑 (Sig1R PAM)，具有認(rèn)知增強(qiáng)效果。體外研究
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.
體內(nèi)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. |