An NMDA receptor antagonist
(+)-MK 801 Maleate 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].
参考文献:
[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.
| In vitro experiment [1]: | |
|
Samples |
Rat cortical slices |
|
Preparation method |
The solubility of this compound in DMSO is > 10.3 mg/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. |
|
Reacting condition |
75 nM; 2 hrs |
|
Applications |
In rat cortical slices, (-)-MK 801 potently blocked N-Me-D-Asp-induced depolarizing responses. At the concentrations of 75 nM and above, (-)-MK 801 irreversibly inhibited N-Me-D-Asp responses and thus, the effect of (-)-MK 801 was persistent. However, (-)-MK 801 acted slowly, reaching its maximal effect only after 90 ~ 120 mins of continuous superfusion. |
| Animal experiment [2]: | |
|
Animal models |
A rat model of ischemic spinal cord injury |
|
Dosage form |
1 mg/kg; i.v. |
|
Applications |
In a rat model of ischemic spinal cord injury, (-)-MK 801 significantly improved neurological outcome and recovery. Moreover, histopathology results showed that (-)-MK 801 reduced injuries in the lumbar gray matter. These results demonstrated that a single dose of (-)-MK 801 given before ischemic spinal cord injury exerted significant neuroprotection effect. |
|
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. |
|
参考文献: [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. [2]. Kocaeli H, Korfali E, Oztürk H, Kahveci N, Yilmazlar S. MK-801 improves neurological and histological outcomes after spinal cord ischemia induced by transient aortic cross-clipping in rats. Surg Neurol. 2005;64 Suppl 2:S22-6; discussion S27. |
|
动态评分
0.0