Saltar al contenido
Merck

M107

Sigma-Aldrich

(+)-MK-801 hydrogen maleate

powder

Sinónimos:

(5S,10R)-(+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine hydrogen maleate, Dizocilpine hydrogen maleate

Iniciar sesiónpara Ver la Fijación de precios por contrato y de la organización


About This Item

Fórmula empírica (notación de Hill):
C16H15N · C4H4O4
Número de CAS:
Peso molecular:
337.37
EC Number:
MDL number:
UNSPSC Code:
12352209
PubChem Substance ID:
NACRES:
NA.32

form

powder

Quality Level

optical activity

[α]25/D +117°, c = 1 in methanol(lit.)

color

white

solubility

DMSO: >20 mg/mL
H2O: 6 mg/mL
0.1 M HCl: soluble
ethanol: soluble

SMILES string

[H]\C(=C(/[H])C(O)=O)C(O)=O.C[C@]12N[C@H](Cc3ccccc13)c4ccccc24

InChI

1S/C16H15N.C4H4O4/c1-16-13-8-4-2-6-11(13)10-15(17-16)12-7-3-5-9-14(12)16;5-3(6)1-2-4(7)8/h2-9,15,17H,10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t15-,16+;/m1./s1

InChI key

QLTXKCWMEZIHBJ-PJGJYSAQSA-N

General description

(+)-MK-801 hydrogen maleate is a highly potent and selective non-competitive NMDA glutamate receptor antagonist that acts at the NMDA receptor-operated ion channel as an open channel blocker. Neurons are depolarized when MK-801 binds to the Glu (40 Glu) receptor (NMDA receptor- ion channel complex) at two sites. 40 Glu is the brain′s primary excitatory neurotransmitter. MK-801 attaches to the ion channel at the binding site PCP of the receptor. Receptor blockade occurs in a voltage-dependent manner. It also known as dizocilpine hydrogen maleate is an effective anticonvulsant with both anxiolytic and sympathomimetic properties.(+)-MK-801 hydrogen maleate stimulates locomotion in monoamine-depleted mice.

Application

(+)-MK-801 hydrogen maleate has been used in following experimental studies:
It is injected to mice to study the effect of systemic administration of CIQ [(3-chlorophenyl) (6, 7-dimethoxy-1-((4-methoxyphenoxy) methyl)-3, 4-dihydroisoquinolin-2(1H)-yl)methanone] on schizophrenia-like behaviours stimulated by MK-801.
It has been used to block the NMDA (N-methyl-D-aspartate) receptor-mediated rtPA (recombinant tissue plasminogen activator)-enhanced excitotoxic pathway.
It is injected in varied doses to study behavioral performance altering effects of MK-801 in zebrafish (Danio rerio).
It is used as a NMDA receptor antagonist to study 3-OH-GA-induced neuronal damage via NMDA receptors.

Biochem/physiol Actions

Experimental study shows that MK-801, influence circling behavior in a direction-specific manner, modify swimming activity and place preference in zebrafish. Acute injection of MK-801, dose dependently, enhances extracellular acetylcholine (ACh) release in the rat parietal cortex. For intracerebral hematomas, MK-801 might act as a potent supplement to reduce delayed edema after recombinant tissue plasminogen activator (rtPA) clot lysis. MK-801 functions as an antidepressant in the social defeat stress model, but it doesn’t have long-lasting effect.
Highly potent and selective non-competitive NMDA glutamate receptor antagonist that acts at the NMDA receptor-operated ion channel as an open channel blocker. Inhibits behavioral sensitization to psychostimulants and ethanol.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

¿Ya tiene este producto?

Encuentre la documentación para los productos que ha comprado recientemente en la Biblioteca de documentos.

Visite la Librería de documentos

Management of delayed edema formation after fibrinolytic therapy for intracerebral hematomas: preliminary experimental data.
Rohde V
Acta Neurochirurgica. Supplement, 105, 101-104 (2008)
Elizabeth K Ruzzo et al.
Cell, 178(4), 850-866 (2019-08-10)
We performed a comprehensive assessment of rare inherited variation in autism spectrum disorder (ASD) by analyzing whole-genome sequences of 2,308 individuals from families with multiple affected children. We implicate 69 genes in ASD risk, including 24 passing genome-wide Bonferroni correction and
Gabrielle Girardeau et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 34(15), 5176-5183 (2014-04-11)
Hippocampal sharp wave-ripples (SPW-Rs) and associated place-cell reactivations are crucial for spatial memory consolidation during sleep and rest. However, it remains unclear how learning and consolidation requirements influence and regulate subsequent SPW-R activity. Indeed, SPW-R activity has been observed not
MK-801 increases endogenous acetylcholine release in the rat parietal cortex: a study using brain microdialysis.
Hasegawa M
Neuroscience Letters, 150(1), 53-56 (1993)
Effects of dizocilpine (MK-801) on circling behavior, swimming activity, and place preference in zebrafish (Danio rerio).
Swain HA
Neurotoxicology and Teratology, 26(6), 725-729 (2004)

Nuestro equipo de científicos tiene experiencia en todas las áreas de investigación: Ciencias de la vida, Ciencia de los materiales, Síntesis química, Cromatografía, Analítica y muchas otras.

Póngase en contacto con el Servicio técnico