地佐环平
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- CAS号:
- 77086-21-6
- 英文名:
- Dizocilpine
- 英文别名:
- C13737;Dizocilpine;MK-801 (Dizocilpine);Dizocilpine (MK-801);Dizocilpine USP/EP/BP;Dizocilpine free base;Dizocilpine free base(MK801);(5S)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5α,10α-imine;(5S,10R)-5-Methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene;5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5S,10R)-
- 中文名:
- 地佐环平
- 中文别名:
- 地卓西平;地佐环平;(5S,10R)-5-甲基-10,11-二氢-5H-5,10-桥亚氨基二苯并[A,D][7]轮烯
- CBNumber:
- CB81075436
- 分子式:
- C16H15N
- 分子量:
- 221.3
- MOL File:
- 77086-21-6.mol
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地佐环平性质、用途与生产工艺
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。
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.
地佐环平
上下游产品信息
上游原料
下游产品
77086-21-6, 地佐环平 相关搜索:
- Inhibitors
- 小分子抑制剂，天然产物
- (5S,10R)-5-甲基-10,11-二氢-5H-5,10-桥亚氨基二苯并[A,D][7]轮烯
- 地卓西平
- 地佐环平
- 77086-21-6
- (5S,10R)-5-Methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene
- Dizocilpine free base
- noncompetitive,MK 801,Dizocilpine,Ionotropic glutamate receptors,voltage,inhibit,MK801,hyperlocomotion,Inhibitor,iGluR,ambulation,neurotransmitter,anticonvulsant
- Dizocilpine (MK-801)
- Dizocilpine USP/EP/BP
- Dizocilpine free base(MK801)
- Dizocilpine
- 5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5S,10R)-
- MK-801 (Dizocilpine)
- C13737
- [5S,10R,(+)]-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5α,10α-imine
- [5S,10R,(+)]-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine
- (5S)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5α,10α-imine