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| | (-)-MK-801 MALEATE Basic information |
| Product Name: | (-)-MK-801 MALEATE | | Synonyms: | (-)-MK-801 MALEATE;(-)-MK 801;(5R)-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine (Z)-2-butenedioate;(5S,10R)-(-)-5-METHYL-10,11-DIHYDRO-5H-DIBENZO[A,D]CYCLOHEPTEN-5,10-IMINE MALEATE;(-)-MK801MALEATE;5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5R,10S)-, (2Z)-2-butenedioate (1:1);MK 801;MK801;C13737;5H-Dibenzo[a,d]cyclohepten-5,10-imine,10,11-dihydro-5-methyl-,(5R,10S) | | CAS: | 121917-57-5 | | MF: | C20H19NO4 | | MW: | 337.37 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 121917-57-5.mol |  |
| | (-)-MK-801 MALEATE Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: >20 mg/mL | | form | solid | | color | white | | Water Solubility | Soluble in water (25mM, gentle warming) |
| Safety Statements | 22-24/25 | | WGK Germany | 3 | | RTECS | HP1093575 |
| | (-)-MK-801 MALEATE Usage And Synthesis |
| 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. |
| | (-)-MK-801 MALEATE Preparation Products And Raw materials |
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