(+)-MK 801 Maleate (Synonyms: Dizocilpine Maleate) |
| رقم الكتالوجGC11025 |
(+)-MK 801 Maleate (MK-801 ماليات) هو مضاد حيوي قوي وانتقائي وغير تنافسي لمستقبلات NMDA مع Kd يبلغ 37.2 نانومتر في غشاء الدماغ للفئران.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 77086-22-7
Sample solution is provided at 25 µL, 10mM.
(+)-MK 801 Maleate is a potent, selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist (Ki = 30.5nM). (+)-MK 801 Maleate has been shown to be protective in various models of ischemia as well as to inhibit behavioral sensitization to certain psychostimulants[1].
(+)-MK 801 Maleate (1.5 and 10μM; 24h) improved the LPS-induced decrease of cell viability in HUVECs. The oxygen consumption, basal and maximal respiration rate, and ATP production in LPS-treated HUVECs were decersed by (+)-MK 801 Maleate (5μM; 2h) via regulating ATP synthesis-related protein SDHB2, MTCO1, and ATP5A[2]. (+)-MK 801 Maleate (500-400μM; 24h) inhibited growth of NSCs in a dose-dependent manner[3].
Acute administration of (+)-MK 801 Maleate (0.1, 0.12, 0.15, 0.2 and 0.3mg/kg; ip; 30 minutes before the test ) increased locomotor activity in the open field test, decreased spontaneous alternations and total arm entries in the Y-maze, and reduced cliff avoidance responses in the cliff avoidance test[4]. A high dose of (+)-MK 801 Maleate (0.1mg/kg; sc; 5d) negatively influenced long-term memory in Wistar rats tested in the radial arm maze, while short-term memory remained unaffected[5]. A single, acute administration of a high (+)-MK 801 Maleate dose (5mg/kg; ip; 4 weeks) in male Wistar rats performing radial maze resulted in deficits of reference but not working spatial memory, and long-term potentiation impairment appeared 7 days and 4 weeks after the injection[6].
References:
[1]. Wong EH, Kemp JA, Priestley T, Knight AR, Woodruff GN, Iversen LL. The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist. Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8.
[2]. Han WM, Hao XB, Hong YX, Zhao SS, Chen XC, Wang R, Wang Y, Li G. NMDARs antagonist MK801 suppresses LPS-induced apoptosis and mitochondrial dysfunction by regulating subunits of NMDARs via the CaM/CaMKII/ERK pathway. Cell Death Discov. 2023 Feb 11;9(1):59.
[3] Ding J, Shao Y, Zhou HH, Ma QR, Zhang YW, Ding YX, He YQ, Liu J. Effect of NMDA on proliferation and apoptosis in hippocampal neural stem cells treated with MK-801. Exp Ther Med. 2018 Aug;16(2):1137-1142.
[4] Mabunga DFN, Park D, Ryu O, Valencia ST, Adil KJL, Kim S, Kwon KJ, Shin CY, Jeon SJ. Recapitulation of Neuropsychiatric Behavioral Features in Mice Using Acute Low-dose MK-801 Administration. Exp Neurobiol. 2019 Dec 31;28(6):697-708.
[5] Svalbe B, Stelfa G, Vavers E, et al. Effects of the N-methyl-d-aspartate receptor antagonist, MK-801, on spatial memory and influence of the route of administration[J]. Behavioural brain research, 2019, 372: 112067.
[6] Janus A, Lustyk K, Pytka K. MK-801 and cognitive functions: Investigating the behavioral effects of a non-competitive NMDA receptor antagonist[J]. Psychopharmacology, 2023, 240(12): 2435-2457.
| Cell experiment [1]: | |
Cell lines | HUVECs |
Preparation Method | HUVECs were pre-incubated with (+)-MK 801 Maleate 5μM for 2h. After incubation of Rhod-2 AM for 30min, cells were exposed to LPS to measure mitochondrial dynamic calcium levels. |
Reaction Conditions | (+)-MK 801 Maleate: 5μM, 2h |
Applications | (+)-MK 801 Maleate restrained LPS-induced mitochondrial dysfunction by regulating mitochondrial membrane potential and mitochondrial Ca2+ uptake. |
| Animal experiment [1]: | |
Animal models | LPS-induced acute lung injury model |
Preparation Method | The mice were randomly assigned to the following three groups: (1) control group; (2) LPS-induced group; and (3) LPS-induced and (+)-MK 801 Maleate-treated group. After 1 week of adaptation to laboratory conditions, LPS (5mg/kg body weight), (+)-MK 801 Maleate1 (10mg/kg body weight), or sterile saline were administered intraperitoneal injection. |
Dosage form | (+)-MK 801 Maleate(10mg/kg; ip; 24h) |
Applications | (+)-MK 801 Maleate can protect mice from LPS-induced acute lung by inhibiting the impairment of vascular permeability. |
References: | |
| Cas No. | 77086-22-7 | SDF | |
| المرادفات | Dizocilpine Maleate | ||
| Chemical Name | (5S,10R)-5-methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene maleate | ||
| Canonical SMILES | C[C@]1(N2)C3=C(C=CC=C3)C[C@@H]2C4=C1C=CC=C4.O=C(O)/C=C\C(O)=O | ||
| Formula | C20H19NO4 | M.Wt | 337.37 |
| الذوبان | ≥ 16.85mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9641 mL | 14.8205 mL | 29.641 mL |
| 5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9641 mL |
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- Purity: >98.00%
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Related Biological Data
Glutamatergic and GABAergic signals to the PVN mediated the anorexic effect of R568 in the AP. (C). Compared with the control group, microinjection of bicuculline and MK-801 alone in the PVN had no significant effect on food intake from 0h to 24h, excluding endogenous effects.
We observed the effect of GABA-A receptor antagonist, ionic blocker of the glutamate NMDAR (MK-801 (GLPBIO, USA), 50nM/0.2µL/mouse; 0.1µL/min), and metabotropic blocker of glutamate receptor I on the action of R568.
Mol Nutr Food Res (2022): 2200245. PMID: 36281915 IF: 6.5749 -
Related Biological Data
Activation of glutamatergic neurons in the BLA by R568 inhibited the synthesis of DA through the NMDAR. (A). VTA pre-injection with MK-801 blocked R568-induced reduction in DA synthesis, whereas pre-injection of LY367385 had no effect on the effect of R568.
MK-801 (GLPBIO, USA)/ LY367385 (MK-801, 50nM 0.2μL−1 per mouse; LY367385, 100nM 0.2μL−1 per mouse) was pre-injected into the ARC/VTA for 20min.
Behavioural Brain Research (2023): 114357. PMID: 36813182 IF: 3.3521
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