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Neuroscience NMDAR Dizocilpine Maleate

Dizocilpine Maleate

Catalog No. T3320   CAS 77086-22-7
Synonyms: (+)-MK 801 (Maleate), (+)-MK 801 maleate, (+)-Mk-801 Hydrogen Maleate, Dizocilpine hydrogen maleate, MK 801

(+)-MK-801 is a potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) with Kd of 37.2 nM in rat brain membranes. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role.

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Dizocilpine Maleate, CAS 77086-22-7
Pack Size Availability Price/USD Quantity
10 mg In stock 50.00
25 mg In stock 82.00
50 mg In stock 149.00
100 mg In stock 268.00
200 mg Inquiry 483.00
1 mL * 10 mM (in DMSO) In stock 50.00
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Purity 99.89%
Purity 99.00%
Purity 99.96%
Biological Description
Chemical Properties
Storage & Solubility Information
Description (+)-MK-801 is a potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) with Kd of 37.2 nM in rat brain membranes. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role.
Targets&IC50 NMDA receptor
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. [4] MK-801 (0.05 mg/kg or 0.2 mg/kg, i.p.) in rats just prior to reactivation of the cocaine-associated memory in the CPP context attenuates subsequent cocaine-primed reinstatement, while no disruption occurres in rats that do not receive reactivation in the CPP context. MK-801 (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage does not suppress subsequent cocaine-primed reinstatement. [5]
Kinase Assay Cerebral cortices from male Sprague-Dawley rats (200-300 g) are homogenized in 9 volumes of ice-cold 0.32mol/Lsucrose by nine strokes with a Teflon/glass homogenizer at 500 rpm. The homogenate is centrifuged for 10 min at 1×103 g, and the supernatant is recentrifuged at 1×104 g for 20 min at 4°C. The pellet is suspended in assay buffer (118 mM NaCl/4.7 mM KCl/1.2mM MgSO4/5 mM NaHCO3/20 mM Hepes/1.2 mM KH2PO4/2.5 mM CaCl2/11 mM glucose, pH 7.4) and incubated at 23°C for 20 min prior to final centrifugation at 1×103 g for 20 min at 4°C. The pellet is resuspended in assay buffer (70 mL per gram of original tissue). Binding of [3H]MK-801 is measured by incubating 750 μL duplicate aliquots of this crude membrane suspension (=0.75 mg of protein) with 100 μL of buffer containing displacer or of buffer alone (total binding), 100 μL of 50 nM [3H]MK-801, and 50 μL of buffer for 60 min at 23°C. Nonspecific binding is defined by 100 μM (final concentration) unlabeled MK-801.
Synonyms (+)-MK 801 (Maleate) , (+)-MK 801 maleate , (+)-Mk-801 Hydrogen Maleate , Dizocilpine hydrogen maleate , MK 801
Purity 99.89%
Molecular Weight 337.38
Formula C20H19NO4
CAS No. 77086-22-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 6 months

Solubility Information

DMSO: 33.7 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
6. Jiang L, et al. Decrease of growth and differentiation factor 10 contributes to neuropathic pain through N-methyl-D-aspartate receptor activation. Neuroreport. 2017 May 24;28(8):444-450.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Neuronal Signaling Compound Library Ion Channel Inhibitor Library Preclinical Compound Library Neurotransmitter Receptor Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Alzheimer's Disease Compound Library

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