中文名 | MK-801 (Dizocilpine) |
英文名 | MK-801 (Dizocilpine) |
别名 | 地佐环平 地卓西平 |
英文别名 | C13737 Dizocilpine MK-801 (Dizocilpine) Dizocilpine free base(MK801) (5S)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5α,10α-imine 5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5S,10R)- [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 |
CAS | 77086-21-6 |
化学式 | C16H15N |
分子量 | 221.3 |
密度 | 1.144±0.06 g/cm3(Predicted) |
熔点 | 68.5-69° |
沸点 | 320.3±11.0 °C(Predicted) |
比旋光度 | 20589 +161.4° (c = 0.038 g/2 ml ethanol) |
酸度系数 | 7.96±0.40(Predicted) |
存储条件 | -20℃ |
体外研究 | 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. |
体内研究 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.519 ml | 22.594 ml | 45.188 ml |
5 mM | 0.904 ml | 4.519 ml | 9.038 ml |
10 mM | 0.452 ml | 2.259 ml | 4.519 ml |
5 mM | 0.09 ml | 0.452 ml | 0.904 ml |
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