地佐环平
| 中文名称 | 地佐环平 |
|---|---|
| 中文同义词 | 地佐环平;地卓西平;(5S,10R)-5-甲基-10,11-二氢-5H-5,10-桥亚氨基二苯并[A,D][7]轮烯 |
| 英文名称 | Dizocilpine |
| 英文同义词 | (5S)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5α,10α-imine;[5S,10R,(+)]-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine;[5S,10R,(+)]-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5α,10α-imine;C13737;MK-801 (Dizocilpine);5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5S,10R)-;Dizocilpine;Dizocilpine free base(MK801) |
| CAS号 | 77086-21-6 |
| 分子式 | C16H15N |
| 分子量 | 221.3 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂，天然产物;Inhibitors |
| Mol文件 | 77086-21-6.mol |
| 结构式 |  |
地佐环平 性质
| 熔点 | 68.5-69° |
|---|---|
| 比旋光度 | 20589 +161.4° (c = 0.038 g/2 ml ethanol) |
| 沸点 | 320.3±11.0 °C(Predicted) |
| 密度 | 1.144±0.06 g/cm3(Predicted) |
| 溶解度 | 溶于 DMSO > 10 mM |
| 形态 | 粉末 |
| 酸度系数(pKa) | 7.96±0.40(Predicted) |
| EPA化学物质信息 | 5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5S,10R)- (77086-21-6) |
Ki: 37.2 nM (NMDA receptor, in rat brain membrane)
Dizocilpine (MK-801) progressively suppresses of current induced by NMDA. Mg
2+
(10 mM) prevents Dizocilpine from blocking the N-Me-D-Asp-induced current, even when Dizocilpine is applied for a long time in the presence of NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches.
Dizocilpine (MK-801; <500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. Dizocilpine (<500 μM) reduces microglial TNF-α output with an EC
50
of 400 μM in BV-2 cells.
Dizocilpine (MK 801) (1 mg/kg) treatment before each METH injection reduces the extent of DA depletion by 55% in striatal of mice. Dizocilpine (MK 801) (1 mg/kg) also attenuates the effects of METH on microglial activation in striatal of mice.
Dizocilpine ((+)-MK 801) (0.05, 0.2 mg/kg, i.p.) attenuates subsequent cocaine-primed reinstatement without disruption in rats. Dizocilpine (MK 801) (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage shows no suppression on subsequent cocaine-primed reinstatement.
Dizocilpine (0.03, 0.1, 0.3 and 1 mg/kg, i.p.) significantly increases the ambulation of mice at 0.3 and 1 mg/kg, but not at 0.03 and 0.1 mg/kg.