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地佐环平

地佐环平 更多供应商
公司名称: 芷威(上海)化学科技有限公司  
联系电话: 021-20221225 13651696729
产品介绍: 英文名称:MK-801 (Dizocilpine)
CAS:77086-21-6
公司名称: 南京康满林化工实业有限公司  
联系电话: 025-83697070
产品介绍: CAS:77086-21-6
纯度:98.00% 包装信息:10g;500g;1kg;10kg 备注:5400/1克;现货
公司名称: BOC Sciences  
联系电话: 16314854226
产品介绍: 英文名称:Dizocilpine
CAS:77086-21-6
公司名称: 上海喀露蓝科技有限公司  
联系电话: 021-64556180 15000803246
产品介绍: 中文名称:地佐环平
英文名称:Dizocilpine
CAS:77086-21-6
纯度:98% 包装信息:1g/;10g/;100g/;1000g/ 备注:1g
公司名称: 上海麦克林生化科技有限公司  
联系电话: 15221275939
产品介绍: 中文名称:地佐环平
英文名称:Dizocilpine
CAS:77086-21-6
纯度:98% (HPLC) 包装信息:25mg
地佐环平
生物活性靶点体外研究体内研究
中文名称:地佐环平
中文同义词:地佐环平;地卓西平
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
地佐环平
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)
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 用途与合成方法
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。
靶点

Ki: 37.2 nM (NMDA receptor, in rat brain membrane)

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.

安全信息
毒害物质数据77086-21-6(Hazardous Substances Data)
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