(+)-MK 801 Maleate (Synonyms: Dizocilpine Maleate) |
| Catalog No.GC11025 |
(+)-MK 801 Maleate es un potente, selectivo y no competitivo antagonista del receptor N-metil-D-aspartato (NMDA) (Ki = 30.5nM). Se ha demostrado que (+)-MK 801 Maleato es protector en varios modelos de isquemia, así como inhibidor de la sensibilización conductual a ciertos psicoestimulantes.
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 es un potente, selectivo y no competitivo antagonista del receptor N-metil-D-aspartato (NMDA) (Ki = 30.5nM). Se ha demostrado que (+)-MK 801 Maleato es protector en varios modelos de isquemia, así como inhibidor de la sensibilización conductual a ciertos psicoestimulantes[1].
(+)-MK 801 Maleato (1.5 y 10μM; 24h) mejoró la viabilidad celular reducida inducida por LPS en HUVECs. El consumo de oxígeno, la tasa de respiración basal y máxima, y la producción de ATP en HUVECs tratadas con LPS fueron reducidos por (+)-MK 801 Maleato (5μM; 2h) mediante la regulación de proteínas relacionadas con la síntesis de ATP, como SDHB2, MTCO1 y ATP5A[2]. (+)-MK 801 Maleato (500-400μM; 24h) inhibió el crecimiento de NSCs de manera dependiente de la dosis[3].
La administración aguda de (+)-MK 801 Maleato (0.1, 0.12, 0.15, 0.2 y 0.3mg/kg; ip; 30 minutos antes de la prueba) aumentó la actividad locomotora en la prueba de campo abierto, disminuyó las alternancias espontáneas y el número total de entradas en el laberinto en Y, y redujo las respuestas de evitación de acantilados en la prueba de evitación de acantilados[4]. Una dosis alta de (+)-MK 801 Maleato (0.1mg/kg; sc; 5d) afectó negativamente la memoria a largo plazo en ratas Wistar probadas en el laberinto radial, mientras que la memoria a corto plazo no se vio afectada[5]. Una administración aguda única de una dosis alta de (+)-MK 801 Maleato (5mg/kg; ip; 4 semanas) en ratas Wistar machos que realizaron el laberinto radial resultó en déficits de memoria espacial de referencia, pero no de trabajo, y se observó deterioro de la potenciación a largo plazo 7 días y 4 semanas después de la inyección[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.
| Experimentos celulares [1]: | |
Líneas celulares | HUVECs |
Método de preparación | Las HUVECs fueron preincubadas con (+)-MK 801 Maleato (5μM) durante 2 horas. Después de la incubación con Rhod-2 AM durante 30 minutos, las células fueron expuestas a LPS para medir los niveles dinámicos de calcio mitocondrial. |
Condiciones de reacción | (+)-MK 801 Maleato: 5μM, 2h |
Áreas de aplicación | (+)-MK 801 Maleato restringió la disfunción mitocondrial inducida por LPS regulando el potencial de la membrana mitocondrial y la captación de Ca2+ mitocondrial. |
| Experimentos con animales [1]: | |
Modelos animales | Modelo de lesión pulmonar aguda inducida por LPS |
Método de preparación | Los ratones fueron asignados aleatoriamente a los siguientes tres grupos: (1) grupo control; (2) grupo inducido por LPS; y (3) grupo inducido por LPS y tratado con (+)-MK 801 Maleato. Después de 1 semana de adaptación a las condiciones de laboratorio, se administraron LPS (5mg/kg de peso corporal), (+)-MK 801 Maleato (10mg/kg de peso corporal) o solución salina estéril mediante inyección intraperitoneal. |
Forma de dosificación | (+)-MK 801 Maleato (10mg/kg; ip; 24h) |
Áreas de aplicación | (+)-MK 801 Maleato puede proteger a los ratones de la lesión pulmonar aguda inducida por LPS inhibiendo el deterioro de la permeabilidad vascular. |
Referencias: [1]. 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. | |
| Cas No. | 77086-22-7 | SDF | |
| Sinónimos | 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 |
| Solubility | ≥ 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. |
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| 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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