Dizocilpine Maleate

SKU: orb1304328

Description

Dizocilpine Maleate (MK-801 maleate) is a potent, selective, non-competitive NMDA receptor antagonist with a Kd of 37.2 nM. It is widely used in neuroscience research to study excitotoxicity, neurodegenerative mechanisms, and to establish pharmacological models of schizophrenia in both in vitro and in vivo experimental systems.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	77086-22-7
MW	337.38
Purity	99.96%
Formula	C₂₀H₁₉NO₄
SMILES	OC(=O)\C=C/C(O)=O.C[C@]12N[C@H](Cc3ccccc13)c1ccccc21
Target	NMDAR,iGluR
Solubility	DMSO:250 mg/mL (741 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.93 mM)

Bioactivity

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Target IC50	NMDAR:37.2 nM(Kd)
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, 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. Read more...
In Vitro	[3H]MK-801 labels high-affinity binding sites in rat cerebral cortical membranes in a saturable manner. MK-801 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 concentration-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. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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noncompetitive, inhibit, Ionotropic glutamate receptors, MK 801, MK 801 Maleate, neurotransmitter, MK-801, MK801, Mk-801 Hydrogen Maleate, MK801 Maleate, MK-801 Maleate, NMDA receptor, iGluR, hyperlocomotion, Inhibitor, Dizocilpine, Dizocilpine hydrogen maleate, Dizocilpine hydrogen Maleate, Dizocilpine Maleate, (+)-MK 801 (Maleate), (+)-MK 801 maleate, (+)-Mk-801 Hydrogen Maleate, ambulation, anticonvulsant, voltage

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Compound Identifiers

PubChem CID

6420042 ↗

Key Properties

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No computed properties available.

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