(-)-MK-801 MALEATE

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

Product Name: (-)-MK-801 MALEATE
CAS No.: 121917-57-5
Chemical Name: (-)-MK-801 MALEATE
Synonyms: CS-2146;(-)-MK 801;(-)-Dizocilpine;(-)-MK801MALEATE;(-)MK-801 maleate;(-)-MK-801 MALEATE;MK 801;MK801;C13737;(-)-DIZOCILPINE MALEATE;(-)-MK-801 MALEATE USP/EP/BP;(-)-Dizocilpine Maleate [(-)-MK 801 maleate
CBNumber: CB5407484
Molecular Formula: C20H19NO4
Formula Weight: 337.37
MOL File: 121917-57-5.mol

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(-)-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)

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Safety

Safety Statements: 22-24/25
WGK Germany: 3
RTECS: HP1093575

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 27213
Product name: (−)-MK-801 (maleate)
Packaging: 10mg
Price: $61
Updated: 2024/03/01

Cayman Chemical

Product number: 27213
Product name: (−)-MK-801 (maleate)
Packaging: 50mg
Price: $243
Updated: 2024/03/01

Cayman Chemical

Product number: 27213
Product name: (−)-MK-801 (maleate)
Packaging: 5mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 27213
Product name: (−)-MK-801 (maleate)
Packaging: 25mg
Price: $139
Updated: 2024/03/01

Tocris

Product number: 0955
Product name: (-)-MK801maleate
Purity: ≥99%(HPLC)
Packaging: 50
Price: $399
Updated: 2021/12/16

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(-)-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

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

Raw materials

Preparation Products

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(-)-MK-801 MALEATE Suppliers

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View Lastest Price from (-)-MK-801 MALEATE manufacturers

Career Henan Chemical Co

Product: (-)-MK801MALEATE 121917-57-5
Price: US $1.00/KG
Min. Order: 1KG
Purity: 99%HPLC
Supply Ability: 100KG
Release date: 2020-02-01

121917-57-5, (-)-MK-801 MALEATERelated Search:

Argatroban (-)-MK 801 MALEATE, >99% (-)-MK 801 MALEATE,(+)-MK 801 MALEATE (-)-MK-801 MALEATE (S)-(-)-N-Benzyl-1-phenylethylamine 1,1-DIMETHYL-1,2,3,4-TETRAHYDROISOQUINOLINE 10,11-DIHYDRO-5 H-DIBENZO[A,D]CYCLOHEPTENE 1-Phenyl-1,2,3,4-tetrahydro-isoquinoline 10,11-dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine ALPHA,ALPHA'-DIMETHYLDIBENZYLAMINE 3-METHYL-1,2,3,4-TETRAHYDROISOQUINOLINE (R)-(+)-N-Benzyl-1-phenylethylamine (2-methylphenyl)(phenyl)methylamine (-)-MK-801 MALEATE

(-)-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)

(-)-DIZOCILPINE MALEATE

CS-2146

(-)MK-801 maleate

(-)-MK-801 MALEATE USP/EP/BP

(-)-Dizocilpine Maleate [(-)-MK 801 maleate

less-active,transporters,()Dizocilpine maleate,Inhibitor,Dizocilpine,inhibit,NMDA,( ) Dizocilpine maleate,monoamine,Ionotropic glutamate receptors,iGluR,antidepressant

(-)-Dizocilpine

(5R,10S)-5-Methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene maleate

121917-57-5

Cell Biology

Cell Signaling and Neuroscience

BioChemical

Ion Channels

Ionotropic Glutamate Receptor Modulators

Ligand-Gated Ion Channels

Inhibitors