ChemicalBook CAS数据库列表 (-)-MK801MALEATE
(-)-MK801MALEATE
- CAS号:121917-57-5
- 英文名:(-)-MK-801 MALEATE
- 中文名:(-)-MK801MALEATE
- CBNumber:CB5407484
- 分子式:C20H19NO4
- 分子量:337.37
- MOL File:121917-57-5.mol
(-)-MK801MALEATE化学性质
- 储存条件 :Store at -20°C
- 溶解度 :DMSO: >20 mg/mL
- 形态 :solid
- 颜色 :white
- 水溶解性 :Soluble in water (25mM, gentle warming)
安全信息
- 安全说明 :22-24/25
- WGK Germany :3
- RTECS号 :HP1093575
(-)-MK801MALEATE性质、用途与生产工艺
- 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。
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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。
(-)-MK801MALEATE上下游产品信息
上游原料
下游产品
(-)-MK801MALEATE 试剂级价格
- 更新日期：2024/11/08
- 产品编号：HY-15084A
- 产品名称：(-)-Dizocilpine maleate
- CAS编号：
- 包装：5 mg
- 价格：290元
- 更新日期：2024/11/08
- 产品编号：HY-15084A
- 产品名称：(-)-MK801MALEATE (-)-Dizocilpine maleate
- CAS编号：121917-57-5
- 包装：10mg
- 价格：465元
(-)-MK801MALEATE生产厂家
- 公司名称：Vinci-Biochem
- 联系电话：--
- 电子邮件：vb@vincibiochem.it
- 国家：意大利
- 产品数：115
- 优势度：58
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