(+)-MK 801
(Synonyms: Dizocilpine maleate;Dizocilpine hydrogen maleate;(+)-MK 801;MK 801) 目录号 : GC16616
强效 NMDA 拮抗剂
Cas No.:70449-94-4
Sample solution is provided at 25 µL, 10mM.
(+)-MK 801 is a potent antagonist of NMDA with Ki value of 30.5nM [1].
MK 801 is a potent anticonvulsant exhibits both anxiolytic and sympathomimetic properties. It is found to be a noncompetitive antagonist of NMDA. MK 801 can penetrate into the central nervous system. In the in vitro assay, MK 801 binds to rat cerebral cortical membrane with high affinity in a saturable manner. This binding is reversible even when the concentration of MK 801 is up to 100μM. It is also found that the binding shows a regional specificity. Most of these binding sites are located in the hippocampus. In rat cortical-slice preparations, MK 801 causes a potent blockade of depolarizing responses to NMDA with a high selectivity. This effect is persistent. The blockade can also cause a suppression of the epileptiform activity induced by tetrodotoxin or other neurotoxin [1].
References:
[1] Wong EH, Kemp JA, Priestley T, Knight AR, Woodruff GN, Iversen LL . The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist. Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8.
| Cell experiment: [1] | |
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Cell lines |
Rat neocortical neurons |
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Preparation method |
The solubility of this compound in DMSO is >10.45mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
10 μM, 11 sec |
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Applications |
Cell was held at -70 mV in the whole-cell recording mode, bathed in the Mg2+-free external solution. Application of 200 μM N-Me-D-Asp elicited an inward current that rose rapidly to a peak and then decayed to a steady current. When N-Me-D-Asp and 10 μM MK-801 were applied simultaneously, the current reached nearly the same peak but was then progressively blocked with a time constant of about 11 sec. The blockade by MK-801 persisted when the cell was washed with control solution for 20 sec. |
| Animal experiment: [2] | |
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Animal models |
Male Wistar rats |
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Dosage form |
Intrathecal injection, 20 μg |
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Applications |
The rats were given morphine (15 μg/h) for 5 days. On day 5 on which tolerance developed, at 3 h after discontinuation of morphine infusion, MK-801 was injected intrathecally 30 min before morphine challenge (15 μg). Pretreatment with MK-801 preserved its antinociceptive effect in morphine-tolerant rats in a dose-dependent manner, with amaximal effect at 60 min. The dose of 10 μg ofMK-801 resulted in only slight preservation of morphine-induced antinociception, while 5 μg of MK-801 had no effect. Injection of 20 μg of MK-801 significantly improved morphine-induced antinociception, with a maximal effect (MPE%) of up to 61%, with a 10 s tail-flick latency being defined as 100% MPE in saline-infused rats. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Huettner J E, Bean B P. Block of N-methyl-D-aspartate-activated current by the anticonvulsant MK-801: selective binding to open channels. Proceedings of the National Academy of Sciences, 1988, 85(4): 1307-1311. [2] Liu C H, Cherng C H, Lin S L, et al. N-methyl-D-aspartate receptor antagonist MK-801 suppresses glial pro-inflammatory cytokine expression in morphine-tolerant rats. Pharmacology Biochemistry and Behavior, 2011, 99(3): 371-380. | |
| Cas No. | 70449-94-4 | SDF | |
| 别名 | Dizocilpine maleate;Dizocilpine hydrogen maleate;(+)-MK 801;MK 801 | ||
| 化学名 | (5S,10R)-5-methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene | ||
| Canonical SMILES | C[C@]1(N2)C3=C(C=CC=C3)C[C@@H]2C4=C1C=CC=C4 | ||
| 分子式 | C16H15N | 分子量 | 221.30 |
| 溶解度 | ≥ 10.45 mg/mL in DMSO, ≥ 102.6 mg/mL in EtOH | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.5188 mL | 22.5938 mL | 45.1875 mL |
| 5 mM | 0.9038 mL | 4.5188 mL | 9.0375 mL |
| 10 mM | 0.4519 mL | 2.2594 mL | 4.5188 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet