地佐环平
- CAS号:77086-21-6
- 英文名:Dizocilpine
- 中文名:地佐环平
- CBNumber:CB81075436
- 分子式:C16H15N
- 分子量:221.3
- MOL File:77086-21-6.mol
- 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 :Soluble in DMSO > 10 mM
- 形态 :Powder
- 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)
地佐环平性质、用途与生产工艺
- 生物活性 Dizocilpine (MK-801),一种有效的抗惊厥剂,是一种选择性非竞争性 NMDA 受体拮抗剂,Kd 为 37.2 nM。Dizocilpine 通过与 NMDA 相关离子通道内的一个位点结合而起作用,从而阻止 Ca2+ 的流动。
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靶点
Ki: 37.2 nM (NMDA receptor, in rat brain membrane)
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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.
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