| 中文名称 | 四氢氨基吖啶 |
| 英文名称 | TACRINE HYDROCHLORIDE |
| CAS号 | 1684-40-8 |
| 分子式 | C13H15ClN2 |
| 分子量 | 234.72 |
| EINECS号 | 216-867-5 |
| 熔点 | 280-284 °C(lit.) |
| 溶解度 | 溶于水性缓冲液 |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | pKa 9.8 (Uncertain) |
| 颜色 | 白色至浅黄色 |
| 危险品标志 | T,Xn |
| 危险类别码 | 25-36/37/38-20/22 |
| 安全说明 | 26-36-45 |
| 危险品运输编号 | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS号 | AR9532500 |
| 危险等级 | 6.1(a) |
| 包装类别 | II |
| 毒性 | LD50 intravenous in mouse: 5600ug/kg |
| Target | Value |
|
BChE
(Cell-free assay) | 25.6 nM |
|
AChE
(Cell-free assay) | 31 nM |
Tacrine (12.5-37.5 nM) inhibits venom acetylcholinesterase as well as human serum butyrylcholinesterase in a concentration-dependent manner.
Tacrine reduces the neurotoxicity induced by the activation of the NMDARs in murine cortical neuronal cultures with an IC
50
of ~500 μM.
Tacrine inhibits the NMDAR responses in a concentration-dependent manner with an IC
50
of ~190 μM at -60 mV.
Tacrine (20-40 μmol/kg; s.c.) disrupts retention of learning in 17- and 30-day old mice in passive avoidance, and while the low dose of tacrine treatment (5 μmol/kg; s.c.) improves retention in 17-day old mice.
Tacrine (0.1-0.4 mg/mL; i.p. for 7 d) inhibits the expression of AChE, but does not significantly improve the protection of the retina function and morphology in mice.
