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(+)-MK 801

Catalog No.
A3100
Potent NMDA antagonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$60.00
In stock
10mg
$50.00
In stock
50mg
$190.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

(+)-MK 801 (CAS: 70449-94-4) is a potent, selective, and non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, displaying a Ki of approximately 30.5 nM. This small molecule readily crosses the blood-brain barrier and interacts reversibly with specific binding sites on cortical membranes, predominantly localized within the hippocampus. In vitro assays utilizing rat cortical slice preparations indicate that (+)-MK 801 robustly inhibits NMDA-induced depolarization events and suppresses epileptiform activity mediated by neurotoxic agents. Due to these pharmacological properties, (+)-MK 801 is utilized experimentally in neuroscience research to study NMDA receptor-mediated events, neurotoxicity, convulsions, and excitatory neurotransmission pathways.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt221.30
Cas No.70449-94-4
FormulaC16H15N
SynonymsDizocilpine maleate;Dizocilpine hydrogen maleate;(+)-MK 801;MK 801
Solubilityinsoluble in H2O; ≥10.45 mg/mL in DMSO; ≥102.6 mg/mL in EtOH
Chemical Name(5S,10R)-5-methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene
SDFDownload SDF
Canonical SMILESC[C@]1(N2)C3=C(C=CC=C3)C[C@@H]2C4=C1C=CC=C4
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment: [1]

Cell lines

Rat neocortical neurons

Preparation method

The solubility of this compound in DMSO is >10.45mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

10 μM, 11 sec

Applications

Cell was held at -70 mV in the whole-cell recording mode, bathed in the Mg2+-free external solution. Application of 200 μM N-Me-D-Asp elicited an inward current that rose rapidly to a peak and then decayed to a steady current. When N-Me-D-Asp and 10 μM MK-801 were applied simultaneously, the current reached nearly the same peak but was then progressively blocked with a time constant of about 11 sec. The blockade by MK-801 persisted when the cell was washed with control solution for 20 sec.

Animal experiment: [2]

Animal models

Male Wistar rats

Dosage form

Intrathecal injection, 20 μg

Applications

The rats were given morphine (15 μg/h) for 5 days. On day 5 on which tolerance developed, at 3 h after discontinuation of morphine infusion, MK-801 was injected intrathecally 30 min before morphine challenge (15 μg). Pretreatment with MK-801 preserved its antinociceptive effect in morphine-tolerant rats in a dose-dependent manner, with amaximal effect at 60 min. The dose of 10 μg ofMK-801 resulted in only slight preservation of morphine-induced antinociception, while 5 μg of MK-801 had no effect. Injection of 20 μg of MK-801 significantly improved morphine-induced antinociception, with a maximal effect (MPE%) of up to 61%, with a 10 s tail-flick latency being defined as 100% MPE in saline-infused rats.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Huettner J E, Bean B P. Block of N-methyl-D-aspartate-activated current by the anticonvulsant MK-801: selective binding to open channels. Proceedings of the National Academy of Sciences, 1988, 85(4): 1307-1311.

[2] Liu C H, Cherng C H, Lin S L, et al. N-methyl-D-aspartate receptor antagonist MK-801 suppresses glial pro-inflammatory cytokine expression in morphine-tolerant rats. Pharmacology Biochemistry and Behavior, 2011, 99(3): 371-380.

Biological Activity

Description (+)-MK 801 is a potent antagonist of NMDA with Ki value of 30.5 nM.
Targets NMDA          
IC50 30.5 nM (Ki)          

Quality Control

Chemical structure

(+)-MK 801 Maleate

Related Biological Data

(+)-MK 801 Maleate