(+)-MK 801 maleate - 10mM in DMSO , CAS No.77086-22-7

CAS: 77086-22-7 Cat. No.: M408185 Molecular Weight: 337.37 EC Number: 278-614-5

GRADE & PURITY 10mM in DMSO

Synonyms

(5S,10R)-(+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine hydrogen maleate

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

(+)-MK-801 is a potent, selective and non-competitiveNMDAreceptor antagonist withKdof 37.2 nM in rat brain membranes.
In vitro

[³H]MK-801 labels high-affinity binding sites in rat cerebral cortical membranes in a saturable manner. MK-801 produces a potent blockade of depolarizing responses to NMDA in rat cerebral cortical slices. The only compounds that are able to compete for [³H]MK-801 binding sites are substances known to block the responses of excitatory amino acids mediated by the NMDA receptor subtype. MK-801 inhibits N-methyl-D-aspartate-induced [³H]norepinephrine (NE) release and [³H]TCP binding in the hippocampus with IC50 of 20 nM and 9 nM, respectively. MK-801 causes a progressive, long-lasting blockade of current induced by NMDA. Mg²⁺ (10 mM) prevents MK-801 from blocking the N-Me-D-Asp-induced current, even when MK-801 is applied for a long time in the presence of NMDA. MK-801 is also effective at blocking NMDA-activated single-channel activity in outside-out patches. MK-801 (< 500 μM) prevents LPS-induced activation of microglia in a concentration-dependent manner with increased Cox-2 protein expression in BV-2 cells. MK-801 (< 500 μM) reduces microglial TNF-α output with EC50 of 400 μM in BV-2 cells.

In vivo

Treatment of mice with MK-801 (1 mg/kg) before each METH injection reduced the extent of DA depletion by 55% in striatal of mice. MK-801 (1 mg/kg) attenuates the effects of METH on microglial activation in striatal of mice. MK-801 (0.05 mg/kg or 0.2 mg/kg, i.p.) in rats just prior to reactivation of the cocaine-associated memory in the CPP context attenuates subsequent cocaine-primed reinstatement, while no disruption occurres in rats that do not receive reactivation in the CPP context. MK-801 (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage does not suppress subsequent cocaine-primed reinstatement.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

(5S, 10R)-(+)-5-Methyl-10, 11-dihydro-5H-dibenzo[a, d]cyclohepten-5, 10-imine hydrogen maleate

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

(+)-MK-801 is a potent, selective and non-competitive NMDA receptor antagonist with K_d of 37.2 nM in rat brain membranes.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

ANTAGONIST

Names and Identifiers

• Pubchem Sid: 488195749
• Pubchem Sid Url: https://pubchem.ncbi.nlm.nih.gov/substance/488195749
• Isomeric SMILES: C[C@@]12C3=CC=CC=C3C[C@@H](N1)C4=CC=CC=C24.C(=C\C(=O)O)\C(=O)O
• Molecular Weight: 337.37
• Reaxy-Rn: 34955296
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=34955296&ln=

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 58 mg/mL (200.43 mM); Ethanol: 58 mg/mL (200.43 mM); Water: Insoluble
• Molecular Weight: 337.400 g/mol
• Hydrogen Bond Donor Count: 3
• Hydrogen Bond Acceptor Count: 5
• Rotatable Bond Count: 2
• Exact Mass: 337.131 Da
• Monoisotopic Mass: 337.131 Da
• Topological Polar Surface Area: 86.600 Ų
• Heavy Atom Count: 25
• Formal Charge: 0
• Complexity: 432.000
• Isotope Atom Count: 0
• Defined Atom Stereocenter Count: 2
• Undefined Atom Stereocenter Count: 0
• Defined Bond Stereocenter Count: 1
• Undefined Bond Stereocenter Count: 0
• The total count of all stereochemical bonds: 1
• Covalently-Bonded Unit Count: 2

XLogP3

References

1. Yue-Heng Yan, Hong-Kun Wang, Zi-Hao Wang, Rui-Ze Wang, Ruo-Xuan Li, Li-Li Huang, Yan-Yan Wang.  (2025)  Effects of anxiety induced by conditioned fear on the expression of NMDA receptors and synaptic plasticity in the rat BLA.  BEHAVIOURAL BRAIN RESEARCH,      [PMID:40132761] [10.1016/j.bbr.2025.115547]

2. Zhengyuan Huang, Guanghui Chen, Zhongyu Ren, Ling Xiao, Ziyue Chen, Yinping Xie, Gaohua Wang, Benhong Zhou.  (2025)  Urolithin A ameliorates schizophrenia-like behaviors and cognitive impairments in female rats by modulating NLRP3 signaling.  INTERNATIONAL IMMUNOPHARMACOLOGY,      [PMID:39987632] [10.1016/j.intimp.2025.114336]

3. Jing Zhang, Yan Zhao.  (2025)  Deficiency of Aldehyde Dehydrogenase 2 Sensitizes cells to Glutamate-Induced Cytotoxicity via Elevation of GluN1 Expression.  TOXICOLOGY,      [PMID:40592419] [10.1016/j.tox.2025.154226]

4. Fan Rui, Pu Jianlin, Zhang Jin, Yu Minglan, Wang Tingting, Geng Xiaoqi, Dong Wei, Ma Rong, Wang Binglong, Wu Jianfei, Liu Kezhi, Hashimoto Kenji, Xiang Bo.  (2025)  Gα13 Overexpression in the Medial Prefrontal Cortex Disrupts Social Behavior Through the Adcyap1/cAMP/PKA/NMDAR Pathway.  SCHIZOPHRENIA BULLETIN,      [PMID:40843621] [10.1093/schbul/sbaf131]

5. Xin Bao, Jingyan Sun, Xing Gao, Mingsheng Xu, Chen Dong, Honghua Pan.  (2026)  A spatiotemporally controlled MNE@PDA-Diz/GP hydrogel system: enhancing spinal cord injury repair via ROS scavenging, calcium influx inhibition, and macrophage polarization.  RSC Advances,  16  (14): (12458-12474).  [PMID:41822204] [10.1039/D5RA08918B]