Identification | Back Directory | [Name]
(-)-MK-801 MALEATE | [CAS]
121917-57-5 | [Synonyms]
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) (5S,10R)-(-)-5-METHYL-10,11-DIHYDRO-5H-DIBENZO[A,D]CYCLOHEPTEN-5,10-IMINE MALEATE (5R)-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine (Z)-2-butenedioate 5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5R,10S)-, (2Z)-2-butenedioate (1:1) | [Molecular Formula]
C20H19NO4 | [MDL Number]
MFCD00082465 | [MOL File]
121917-57-5.mol | [Molecular Weight]
337.37 |
Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: >20 mg/mL
| [form ]
solid
| [color ]
white
| [Water Solubility ]
Soluble in water (25mM, gentle warming) |
Hazard Information | Back Directory | [Uses]
(-)-MK 801 Maleate was used in biological study to observe antipsychotics and other agents effects on prepulse inhibition of acoustic startle in rats. Binding properties of (-)-MK 801 Maleate, NMDA receptor channel blocker, were characterized in different brain regions | [Biological Activity]
(+)-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]. | [in vitro]
[3H]MK-801 labels high-affinity binding sites in rat cerebral cortical membranes in a saturable manner. It 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 conce ntration-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. | [in vivo]
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, ip) in rats just prior to reactivation of the cocaine-associated memory in the CPP context attenuates subsequent cocaine-primed reinstatement, while no disruption occurs in rats that do not receive reactivation in the CPP context. MK-801 (0.2 mg/kg, ip) prior to two reactivation sessions in the home cage does not suppress subsequent cocaine-primed reinstatement. | [target]
Target | Value | NMDA receptor | 30.5 nM(Ki) |
| [storage]
Room temperature | [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. |
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