MK 801
(-)-MK 801 Maleate
CAS: 121917-57-5
Molecular Formula: C20H19NO4
MK 801 - Names and Identifiers
MK 801 - Physico-chemical Properties
| Molecular Formula | C20H19NO4 |
| Molar Mass | 337.37 |
| Solubility | DMSO: >20mg/mL |
| Appearance | solid |
| Color | white |
| Storage Condition | -20℃ |
| In vitro study | [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 [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) Prevent LPS-induced activation of microglia in a concentration-dependent manner with increased Cox-2 protein expression in BV-2 cells. MK-801 (< 500 μm) reductions microglia TNF-α output with EC50 of 400 μm in BV-2 cells. In vitro neurophysiological studies using a rat cortical slice preparation, demonstrated potent, selective, non-competitive antagonism of dizocilpine to a N-Me-D-Asp depolarization response, however, there was no such effect on kainic acid or plasmacine. The efficacy of enantiomers of Phencyclidine,ketamine,SKF 10047, and diazocilpine as N-Me-D-Asp antagonists is closely related to their efficacy as [3H] diazocilpine binding inhibitors. This indicates that the dizocilpine binding site is associated with the N-Me-D-Asp receptor and explains the mechanism of action of dizocilpine as an antispasmodic agent. |
| In vivo study | 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 Corona-associated memory in the CPP context. MK-801 (0.2 mg/kg, I. p.) prior to two reactivation sessions in the home cage does. after spinal cord ischemic injury (ISCI), all rats in the control group had severe permanent nerves Functional deficits, while rats treated with dizocilpine had statistically (P < .05) better neurological function and recovered well. Histopathology showed severe Neuronal necrosis in the lumbar gray matter of control rats, whereas dizocilpine treated rats showed only mild damage. These results indicate that single dose administration of dizocilpine prior to ISCI provided significant neuroprotective effect. |
MK 801 - Risk and Safety
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| RTECS | HP1093575 |
MK 801 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.964 ml | 14.821 ml | 29.641 ml |
| 5 mM | 0.593 ml | 2.964 ml | 5.928 ml |
| 10 mM | 0.296 ml | 1.482 ml | 2.964 ml |
| 5 mM | 0.059 ml | 0.296 ml | 0.593 ml |
Last Update：2024-01-02 23:10:35
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