(+)-MK 801
(+)-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.
- 1. Jing Chen, Hong-Wei Sun, et al. "Glutamate promotes CCL2 expression to recruit tumor-associated macrophages by restraining EZH2-mediated histone methylation in hepatocellular carcinoma." Oncoimmunology. 2025 Dec;14(1):2497172. PMID: 40271976
- 2. Teng Xu, Taotao Zhou, et al. "MouseGPT: A Large-scale Vision-Language Model for Mouse Behavior Analysis." bioRxiv. April 01, 2025.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 221.30 |
| Cas No. | 70449-94-4 |
| Formula | C16H15N |
| Synonyms | Dizocilpine maleate;Dizocilpine hydrogen maleate;(+)-MK 801;MK 801 |
| Solubility | insoluble 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 |
| SDF | Download SDF |
| Canonical SMILES | C[C@]1(N2)C3=C(C=CC=C3)C[C@@H]2C4=C1C=CC=C4 |
| Shipping Condition | Small 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. |
| 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. |
|
| 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 & MSDS
- View current batch:
Chemical structure
Related Biological Data
