ArticleBiophysical journal1994
Interaction of the NMDA receptor noncompetitive antagonist MK-801 with model and native membranes.
Article in Biophysical journal, 1994. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 16 citations in OpenAlex.
- Pharmacological inhibition of NMDA receptors reduces migration and viability in triple-negative inflammatory breast cancer cell lines.Discover oncology · 2025Article
- Dietary Plant Polyphenols as the Potential Drugs in Neurodegenerative Diseases: Current Evidence, Advances, and Opportunities.Oxidative medicine and cellular longevity · 2022Review
- Prefrontal inhibition of neuronal KBritish journal of pharmacology · 2020Article
- Polarity of Hydrated Phosphatidylcholine Headgroups.Langmuir : the ACS journal of surfaces and colloids · 2019Article
- Vesicular glutamate release from central axons contributes to myelin damage.Nature communications · 2018Article
- Retrieval-induced NMDA receptor-dependent Arc expression in two models of cocaine-cue memory.Neurobiology of learning and memory · 2014Article
- Structure-based prediction of drug distribution across the headgroup and core strata of a phospholipid bilayer using surrogate phases.Molecular pharmaceutics · 2014Article
- Common influences of non-competitive NMDA receptor antagonists on the consolidation and reconsolidation of cocaine-cue memory.Psychopharmacology · 2013Article
- Molecular mechanisms of excitotoxicity and their relevance to pathogenesis of neurodegenerative diseases.Acta pharmacologica Sinica · 2009Review
- Partitioning of organic compounds in phases imitating the headgroup and core regions of phospholipid bilayers.Langmuir : the ACS journal of surfaces and colloids · 2006Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
MK-801, a noncompetitive antagonist of the NMDA (N-methyl-D-aspartate) receptor, has protective effects against excitotoxicity and ethanol withdrawal seizures. We have determined membrane/buffer partition coefficients (Kp[mem]) of MK-801 and its rates of association with and dissociation from membranes. Kp[mem] (+/- SD) = 1137 (+/- 320) in DOPC membranes and 485 (+/- 99) in synaptoneurosomal (SNM) lipid membranes from rat cerebral cortex (unilamellar vesicles). In multilamellar vesicles, Kp[mem] was higher: 3374 (+/- 253) in DOPC and 6879 (+/- 947) in SNM. In cholesterol/DOPC membranes, Kp[mem] decreased as the cholesterol content increased. MK-801 associated with and dissociated from membranes rapidly. Addition of ethanol to SNM did not affect Kp[mem]. MK-801 decreased the cooperative unit size of DMPC membranes. The decrease was smaller than that caused by 1,4-dihydropyridine drugs, indicating a weaker interaction with the hydrocarbon core. Small angle x-ray diffraction, with multilayer autocorrelation difference function modeling, indicated that MK-801 in a cholesterol/DOPC membrane (mole ratio = 0.6) causes a perturbation at approximately 16.0 A from the bilayer center. In bilayers of cholesterol/DOPC = 0.15 (mole ratio) or pure DOPC, the perturbation caused by MK-801 was more complex. The physical chemical interactions of MK-801 with membranes in vitro are consistent with a fast onset and short duration of action in vivo.
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Registered trials
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