(+)-Dizocilpine (MK 801) Maleate

Catalog No.S2876

For research use only.

(+)-Dizocilpine (MK 801) Maleate is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.

(+)-Dizocilpine (MK 801) Maleate Chemical Structure

CAS No. 77086-22-7

Selleck's (+)-Dizocilpine (MK 801) Maleate has been cited by 7 Publications

Purity & Quality Control

Choose Selective NMDAR Inhibitors

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 Research:

[4]

  • Animal Models: Male Sprague-Dawley and Long-Evans Hooded rats
  • Dosages: 0.2 mg/kg
  • Administration: Intraperitoneal injection

Solubility (25°C)

In vitro

DMSO 68 mg/mL
(201.55 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 337.37
Formula

C16H15N.C4H4O4

CAS No. 77086-22-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC12C3=CC=CC=C3CC(N1)C4=CC=CC=C24.C(=CC(=O)O)C(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy (+)-Dizocilpine (MK 801) Maleate | (+)-Dizocilpine (MK 801) Maleate supplier | purchase (+)-Dizocilpine (MK 801) Maleate | (+)-Dizocilpine (MK 801) Maleate cost | (+)-Dizocilpine (MK 801) Maleate manufacturer | order (+)-Dizocilpine (MK 801) Maleate | (+)-Dizocilpine (MK 801) Maleate distributor