(+)-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.
(+)-MK 801 Maleate是一种强效、选择性和非竞争性的 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂 (Ki = 30.5nM)。(+)-MK 801 Maleate已被证明在各种缺血模型中具有保护作用，并能抑制对某些精神兴奋剂的行为敏感化[1]。
(+)-MK 801 Maleate（1、5、10μM；24h）改善了LPS诱导的HUVEC细胞活力下降。(+)-MK 801 Maleate（5μM，2h）通过调节 ATP 合成相关蛋白SDHB2、MTCO1和ATP5A，减少LPS诱导的HUVEC的耗氧量、基础和最大呼吸速率以及ATP生成[2]。(+)-MK 801 Maleate（500-400μM；24h）以剂量依赖性方式抑制NSC细胞的生长[3]。
(+)-MK 801 Maleate（0.1、0.12、0.15、0.2 、0.3mg/kg；ip；测试前30分钟）可增加旷场测试中的运动活动，减少Y型迷宫中的自发交替和总进臂次数，并减少悬崖回避测试中的悬崖回避反应[4]。(+)-MK 801 Maleate（0.1mg/kg；SC；5d）对在放射臂迷宫中测试的Wistar大鼠的长期记忆产生负面影响，而短期记忆不受影响[5]。对雄性Wistar大鼠进行放射状迷宫测试时，单次急性注射高剂量(+)-MK 801 Maleate（5mg/kg；ip；4 weeks）导致参考记忆丧失，但空间记忆正常，并且在注射后7天和4周出现长期增强障碍[6]。