M107

(+)-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
• Fórmula empírica (notación de Hill): C₁₆H₁₅N · C₄H₄O₄
• Número de CAS: 77086-22-7
• Peso molecular: 337.37
• Número CE: 278-614-5
• Número MDL: MFCD00082465
• Código UNSPSC: 12352209
• ID de la sustancia en PubChem: 24277988
• NACRES: NA.32

Propiedades

• Formulario: powder
• Nivel de calidad: 100
• actividad óptica: [α]25/D +117°, c = 1 in methanol(lit.)
• color: white
• solubilidad: DMSO: >20 mg/mL; H₂O: 6 mg/mL; 0.1 M HCl: soluble; ethanol: soluble
• cadena SMILES: [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
• Clave InChI: QLTXKCWMEZIHBJ-PJGJYSAQSA-N
• Información sobre el gen: human ... GRIN1(2902) , GRIN2A(2903) , GRIN2B(2904) , GRIN2C(2905) , GRIN2D(2906) , GRIN3A(116443) , GRIN3B(116444) , GRINA(2907) ; mouse ... GRIN1(14810) , GRIN2A(14811) , GRIN2B(14812) , GRIN2C(14813) , GRIN2D(14814) , GRIN3A(242443) , GRIN3B(170483) , GRINA(66168) ; rat ... GRIN1(24408) , GRIN2A(24409) , GRIN2B(24410) , GRIN2C(24411) , GRIN2D(24412) , GRIN3A(191573) , GRIN3B(170796) , GRINA(266668)

Descripción

Descripción general

(+)-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.[1] It also known as dizocilpine hydrogen maleate is an effective anticonvulsant with both anxiolytic and sympathomimetic properties.[2](+)-MK-801 hydrogen maleate stimulates locomotion in monoamine-depleted mice.[3]

Aplicación

(+)-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.[4]
It has been used to block the NMDA (N-methyl-D-aspartate) receptor-mediated rtPA (recombinant tissue plasminogen activator)-enhanced excitotoxic pathway.[5]
It is injected in varied doses to study behavioral performance altering effects of MK-801 in zebrafish (Danio rerio).[6]
It is used as a NMDA receptor antagonist to study 3-OH-GA-induced neuronal damage via NMDA receptors.[7]

Acciones bioquímicas o fisiológicas

Experimental study shows that MK-801, influence circling behavior in a direction-specific manner, modify swimming activity and place preference in zebrafish.[8] Acute injection of MK-801, dose dependently, enhances extracellular acetylcholine (ACh) release in the rat parietal cortex.[9] For intracerebral hematomas, MK-801 might act as a potent supplement to reduce delayed edema after recombinant tissue plasminogen activator (rtPA) clot lysis.[5] MK-801 functions as an antidepressant in the social defeat stress model, but it doesn’t have long-lasting effect.[10]

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.

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable
• Equipo de protección personal: Eyeshields, Gloves, type N95 (US)