(+)-MK 801 Maleate (Synonyms: Dizocilpine Maleate) |
| Catalog No.GC11025 |
(+)-MK 801 Maleate는 강력하고 선택적이고 비경쟁적인 N-methyl-D-aspartate (NMDA) 수용체 싸이어(Ki = 30.5nM)이다. (+)-MK 801 Maleate는 다양한 뇌혈액 모델에서 보호 작용을 보이고 일부 정신 자극제에 대한 행동 민감화를 억제하는 것으로 나타났다.
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 Maleate는 강력하고 선택적이고 비경쟁적인 N-methyl-D-aspartate (NMDA) 수용체 싸이어(Ki = 30.5nM)이다. (+)-MK 801 Maleate는 다양한 뇌혈액 모델에서 보호 작용을 보이고 일부 정신 자극제에 대한 행동 민감화를 억제하는 것으로 나타났다.
(+)-MK 801 Maleate (1.5와 10μM; 24시간)는 LPS 유도된 HUVECs 세포 활성 저하를 개선했다. (+)-MK 801 Maleate (5μM; 2시간)는 ATP 합성과 관련된 단백질 SDHB2, MTCO1, ATP5A를 조절하여 LPS 처리된 HUVECs의 산소 소비, 기초 및 최대 호흡 속도, ATP 생산을 낮췄다[2]. (+)-MK 801 Maleate (500-400μM; 24시간)는 용량 의존적으로 NSCs의 성장을 억제하는 방식으로 작용했다[3].
급성 투여 (+)-MK 801 Maleate (0.1, 0.12, 0.15, 0.2 및 0.3mg/kg; ip; 시험 30분 전)가 오픈 필드 테스트에서의 활동성을 증가시켰고 Y-미로에서의 자발적 교대로동과 총 팔굽이 수를 줄였고 클리프 회피 테스트에서의 클리프 회피 반응을 감소시켰다[4]. 고용량의 (+)-MK 801 Maleate (0.1mg/kg; sc; 5일)가 레이디얼 암 마지막에서 시험된 위스타트 쥐의 장기 기억에 부정적인 영향을 미친 반면 단기 기억은 영향을 받지 않았다[5]. 급성 고용량의 (+)-MK 801 Maleate 투여 (5mg/kg; ip; 4주)가 레이디얼 미로에서 시험된 수컷 위스타트 쥐에서 참조 공간 기억의 결함을 일으켰고 작업 공간 기억에는 영향을 미치지 않았다. 장기 강화 장애는 주사 후 7일과 4주에 나타났다[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.
| 세포 실험 [1]: | |
세포 라인 | HUVECs |
제조 방법 | HUVECs를 5μM의 (+)-MK 801 Maleate와 사전 배양하여 2시간 동안 배양했습니다. Rhod-2 AM으로 30분 동안 배양한 후 세포는 LPS에 노출되어 미토콘드리아 동적 칼슘 수준을 측정하기 위해 사용되었습니다. |
반응 조건 | (+)-MK 801 Maleate: 5μM, 2 시간 동안 |
응용 분야 | (+)-MK 801 Maleate는 미토콘드리아 막전위와 미토곤드리아 Ca2+ 흡수를 조절하여 LPS 유도된 미토콘드리아 기능 장애를 억제했습니다. |
| 동물 실험 [2]: | |
동물 모형 | LPS로 유발된 급성 폐 손상 모델 |
제조 방법 | 쥐가 다음 세 그룹으로 무작위로 배정되었습니다: (1)대조 그룹; (2) LPS 유도 그룹; (3) LPS 유도 및 (+)-MK 801 Maleate 치료 그룹. 실험실 조건에 1주일간 적응한 후 LPS(5mg/kg 체중), (+)-MK 801 Maleate 1(10mg/kg 체중), 또는멸균 식염수를 복간 주사로 투여했습니다. |
제형 | (+)-MK 801 Maleate(10mg/kg; ip; 24시간 동안) |
응용 분야 | (+)-MK 801 Maleate는 혈관 투과성의 손상을 억제하여 쥐를 LPS 유도된 급성 폐 손상으로부터 보호할 수 있습니다. |
References: | |
| Cas No. | 77086-22-7 | SDF | |
| Synonyms | 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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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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