(+)-Dizocilpine (MK 801) Maleate

Catalog No.S2876 Batch:S287601

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Technical Data

Formula

C16H15N.C4H4O4
Molecular Weight 337.37 CAS No. 77086-22-7
Solubility (25°C)* In vitro DMSO 68 mg/mL (201.55 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.4mg/ml Taking the 1 mL working solution as an example, add 50 μL of 68 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% corn oil
1.7mg/ml Taking the 1 mL working solution as an example, add 50 μL of 34 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description (+)-Dizocilpine (MK 801) Maleate is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
Targets
NMDA receptor [1]
37.2 nM(Kd)
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. [1] 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. [2] 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. [3] 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. [4]
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]

Protocol (from reference)

Animal Study:

[4]
  • Animal Models

    Male Sprague-Dawley and Long-Evans Hooded rats

  • Dosages

    0.2 mg/kg

  • Administration

    Intraperitoneal injection

Selleck's (+)-Dizocilpine (MK 801) Maleate has been cited by 11 publications

Sevoflurane upregulates neuron death process-related Ddit4 expression by NMDAR in the hippocampus [ Aging -Albany NY), 2023, 15(12):5698-5712] PubMed: 37348034
Sevoflurane upregulates neuron death process-related Ddit4 expression by NMDAR in the hippocampus [ Aging (Albany NY), 2023, 15(12):5698-5712] PubMed: 37348034
N-Methyl D-aspartate receptor subtype 2B/Ca2+/calmodulin-dependent protein kinase II signaling in the lateral habenula regulates orofacial allodynia and anxiety-like behaviors in a mouse model of trigeminal neuralgia [ Front Cell Neurosci, 2022, 16:981190] PubMed: 36187288
Functionally distinct roles for eEF2K in the control of ribosome availability and p-body abundance [ Nat Commun, 2021, 12(1):6789] PubMed: 34815424
Unraveling Autocrine Signaling Pathways through Metabolic Fingerprinting in Serous Ovarian Cancer Cells [ Biomedicines, 2021, 9(12)1927] PubMed: 34944743
Lipid bilayers regulate allosteric signal of NMDA receptor GluN1 C-terminal domain [ Biochem Biophys Res Commun, 2021, 585:15-21] PubMed: 34781056
Evaluation of acute and chronic nociception in subchronically administered MK-801-induced rat model of schizophrenia [ Behav Pharmacol, 2021, 32(7):571-580] PubMed: 34494988
Bivalves are NO different: nitric oxide as negative regulator of metamorphosis in the Pacific oyster, Crassostrea gigas [ BMC Dev Biol, 2020, 20(1):23] PubMed: 33228520
Propofol attenuates the adhesion of tumor and endothelial cells through inhibiting glycolysis in human umbilical vein endothelial cells. [ Acta Biochim Biophys Sin (Shanghai), 2019, 51(11):1114-1122] PubMed: 31650167
Activation of the N-methyl-d-aspartate receptor is involved in glyphosate-induced renal proximal tubule cell apoptosis [ J Appl Toxicol, 2019, 39(8):1096-1107] PubMed: 30907447

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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