121917-57-5
中文名称
(-)-MK801MALEATE
英文名称
(-)-MK-801 MALEATE
CAS
121917-57-5
分子式
C20H19NO4
分子量
337.37
MOL 文件
121917-57-5.mol
更新日期
2024/04/22 19:32:15
121917-57-5 结构式
基本信息
中文别名
顺丁烯二酸盐 (-)-MK(-)-MK 801马来酸
(-)-MK801 马来酸盐
英文别名
CS-2146(-)-MK 801
(-)-MK801MALEATE
(-)MK-801 maleate
(-)-MK-801 MALEATE
MK 801
MK801
C13737
(-)-DIZOCILPINE MALEATE
(-)-MK-801 MALEATE USP/EP/BP
(-)-Dizocilpine Maleate [(-)-MK 801 maleate
5H-Dibenzo[a,d]cyclohepten-5,10-imine,10,11-dihydro-5-methyl-,(5R,10S)
所属类别
生物化工：GluR 拮抗剂物理化学性质
储存条件-20°C储存
溶解度DMSO: >20 mg/mL
溶解度二甲基亚砜：>20 mg/mL
形态solid
颜色white
水溶解性Soluble in water (25mM, gentle warming)
常见问题列表
生物活性
(-)-MK 801 Maleate作用于大鼠脑组织膜，是一种有效的，选择性的，非竞争性NMDA受体拮抗剂，Kd为37.2 nM。体外研究
[3H]MK-801 labels high-affinity binding sites in rat cerebral cortical membranes in a saturable manner. MK-801 produces a potent blockade of depolarizing responses to NMDA in rat cerebral cortical slices. The only compounds that are able to compete for [3H]MK-801 binding sites are substances known to block the responses of excitatory amino acids mediated by the NMDA receptor subtype. MK-801 inhibits N-methyl-D-aspartate-induced [3H]norepinephrine (NE) release and [3H]TCP binding in the hippocampus with IC50 of 20 nM and 9 nM, respectively. MK-801 causes a progressive, long-lasting blockade of current induced by NMDA. Mg2+ (10 mM) prevents MK-801 from blocking the N-Me-D-Asp-induced current, even when MK-801 is applied for a long time in the presence of NMDA. MK-801 is also effective at blocking NMDA-activated single-channel activity in outside-out patches. MK-801 (< 500 μM) prevents LPS-induced activation of microglia in a concentration-dependent manner with increased Cox-2 protein expression in BV-2 cells. MK-801 (< 500 μM) reduces microglial TNF-α output with EC50 of 400 μM in BV-2 cells.体内研究
Treatment of mice with MK-801 (1 mg/kg) before each METH injection reduced the extent of DA depletion by 55% in striatal of mice. MK-801 (1 mg/kg) attenuates the effects of METH on microglial activation in striatal of mice. MK-801 (0.05 mg/kg or 0.2 mg/kg, i.p.) in rats just prior to reactivation of the cocaine-associated memory in the CPP context attenuates subsequent cocaine-primed reinstatement, while no disruption occurres in rats that do not receive reactivation in the CPP context. MK-801 (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage does not suppress subsequent cocaine-primed reinstatement.生物活性
(-)-MK-801 (Dizocilpine, C13737) 是一种有效的N-methyl-D-aspartate(NMDA)受体拮抗剂，Ki为30.5 nM。靶点
| Target | Value |
| NMDA receptor | 30.5 nM(Ki) |
体外研究
体外神经生理学研究使用大鼠皮质切片制剂，证明了dizocilpine对N-Me-D-Asp去极化响应具有有效的，选择性的，非竞争性的拮抗作用，但是对红藻氨酸或使君子氨酸无此作用。Phencyclidine，ketamine，SKF 10047，和dizocilpine的对映异构体，作为N-Me-D-Asp拮抗剂的效能与它们作为[3H] dizocilpine结合抑制剂的效能密切相关。这表明，dizocilpine结合位点与N-Me-D-Asp受体相关，并解释了dizocilpine作为抗痉挛剂的作用机制。
体内研究
在脊髓缺血性损伤(ISCI)后，所有对照组大鼠患有严重的永久性神经功能缺损，而dizocilpine治疗的大鼠具有统计学上(P < .05)更好的神经功能，并且恢复良好。组织病理学表明对照组大鼠的腰灰质出现严重的神经元坏死，而dizocilpine处理的大鼠仅表现出轻度损伤。这些结果表明，ISCI 之前，dizocilpine单剂量给药提供显著的神经保护作用。