ChemicalBook > CAS DataBase List > (-)-MK-801 MALEATE

(-)-MK-801 MALEATE

(-)-MK-801 MALEATE Structure
(-)-MK-801 MALEATE
  • CAS No.121917-57-5
  • Chemical Name:(-)-MK-801 MALEATE
  • CBNumber:CB5407484
  • Molecular Formula:C20H19NO4
  • Formula Weight:337.37
  • MOL File:121917-57-5.mol
(-)-MK-801 MALEATE Property
  • storage temp. Store at -20°C
  • solubility DMSO: >20 mg/mL
  • form solid
  • color white
  • Water Solubility Soluble in water (25mM, gentle warming)
  • FDA UNII EF13O02IV0
Safety
  • Safety Statements  :22-24/25
  • WGK Germany  :3
  • RTECS  :HP1093575
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal word
  • Hazard statements
  • Precautionary statements

(-)-MK-801 MALEATE Chemical Properties,Usage,Production

  • 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
    TargetValue
    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
Raw materials
Preparation Products
(-)-MK-801 MALEATE Suppliers
Global(134)Suppliers
  • Supplier：
    career henan chemical co
  • Tel：+86-0371-86658258<br/>+8613203830695
  • Email：factory@coreychem.com
  • Country：China
  • ProdList：29807
  • Advantage：58
  • Supplier：
    Xi'an MC Biotech, Co., Ltd.
  • Tel：029-89275612<br/>+8618991951683
  • Email：mcbio_sales@163.com
  • Country：China
  • ProdList：2251
  • Advantage：58
  • Supplier：
    InvivoChem
  • Tel：+1-708-310-1919<br/>+1-13798911105
  • Email：sales@invivochem.cn
  • Country：United States
  • ProdList：6391
  • Advantage：58
  • Supplier：
    LEAP CHEM CO., LTD.
  • Tel：+86-852-30606658
  • Email：market18@leapchem.com
  • Country：China
  • ProdList：24727
  • Advantage：58
(-)-MK-801 MALEATE Spectrum
121917-57-5, (-)-MK-801 MALEATERelated Search:
  • Inhibitors
  • 抑制剂
  • 药靶配体
  • 小分子抑制剂，天然产物
  • 神经信号
  • Ligand-Gated Ion Channels
  • Ionotropic Glutamate Receptor Modulators
  • Ion Channels
  • BioChemical
  • Cell Signaling and Neuroscience
  • Cell Biology
  • (-)-MK 801马来酸,10 MM DMSO 溶液
  • (5R,10S)-5-甲基-10,11-二氢-5H-5,10-EPIMINO二苯并[A,D][7]环庚烯 马来酸盐
  • 优选](-)-MK 801
  • 顺丁烯二酸盐 (-)-MK
  • (-)-MK 801马来酸
  • (-)-MK801 马来酸盐
  • 121917-57-5
  • (-)-Dizocilpine (MK 801) Maleate
  • (-)-MK 801 maleate (-)-Dizocilpine maleate
  • (-)-Dizocilpine maleate, 10 mM in DMSO
  • (5R,10S)-5-Methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene maleate
  • (-)-Dizocilpine
  • less-active,transporters,()Dizocilpine maleate,Inhibitor,Dizocilpine,inhibit,NMDA,( ) Dizocilpine maleate,monoamine,Ionotropic glutamate receptors,iGluR,antidepressant
  • (-)-Dizocilpine Maleate [(-)-MK 801 maleate
  • (-)-MK-801 MALEATE USP/EP/BP
  • (-)MK-801 maleate
  • CS-2146
  • (-)-DIZOCILPINE MALEATE
  • 5H-Dibenzo[a,d]cyclohepten-5,10-imine,10,11-dihydro-5-methyl-,(5R,10S)
  • MK 801;MK801;C13737
  • 5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5R,10S)-, (2Z)-2-butenedioate (1:1)
  • (-)-MK801MALEATE
  • (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
  • (-)-MK 801
  • (-)-MK-801 MALEATE

Home

My