Felbamate block of recombinant N-methyl-d-aspartate receptors: selectivity for the NR2B subunit
@article{Harty2000FelbamateBO, title={Felbamate block of recombinant N-methyl-d-aspartate receptors: selectivity for the NR2B subunit}, author={T. Patrick Harty and Michael A. Rogawski}, journal={Epilepsy Research}, year={2000}, volume={39}, pages={47-55} }
79 Citations
Mechanisms of NMDA receptor inhibition by nafamostat, gabexate and furamidine.
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The N-methyl-D-aspartate receptor subunit NR2B: localization, functional properties, regulation, and clinical implications.
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- 2003
Molecular determinants of the anticonvulsant felbamate binding site in the N-methyl-D-aspartate receptor.
- BiologyJournal of medicinal chemistry
- 2008
It is concluded that residues L643 and T647 in NR2B as well as homologous residues V644 and T648 in NR1 are the major, and very likely the exclusive, molecular determinants constituting the FBM binding site in the NMDA receptor.
Characterization of the gating conformational changes in the felbamate binding site in NMDA channels.
- BiologyBiophysical journal
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It is suggested that the effects of NMDA and glycine binding coalesce or are interrelated before or at the actual activation gate, and FBM binding seems to modulate NMDA channel gating at or after this coalescing point.
Extracellular proton-modulated pore-blocking effect of the anticonvulsant felbamate on NMDA channels.
- BiologyBiophysical journal
- 2007
FBM therefore acts as an opportunistic pore blocker modulated by extracellular proton, suggesting that the FBM binding site is located at the junction of a widened and a narrow part of the ion conduction pathway.
REPLY
- Biology
- 2000
Felbamate is the only marketed anticonvulsant agent with unequivocal NMDA receptor blocking activity at clinically relevant concentrations and Mazarati et al. are to be commended for highlighting the potential utility of felbamate and otherNMDA receptor antagonists in the termination of status epilepticus and for protecting against the associated seizure-induced brain damage.
Felbamate is a subunit selective modulator of recombinant gamma-aminobutyric acid type A receptors expressed in Xenopus oocytes.
- BiologyEuropean journal of pharmacology
- 2006
Mechanisms of NMDA receptor inhibition by diarylamidine compounds
- Biology, ChemistryThe European journal of neuroscience
- 2019
Dinazene and DAPI demonstrated tail currents and overshoots suggesting “foot‐in‐the‐door” mechanism of action, and pentamidine was partially trapped in the closed NMDA receptor channels, which can be explained by the difference in the 3D structure of compounds.
Enhanced glutamatergic transmission reduces the anticonvulsant potential of lamotrigine but not of felbamate against tonic-clonic seizures.
- Biology, PsychologyPharmacological reports : PR
- 2007
It is indicated that felbamate, but not lamotrigine, effectively prevents generalized tonic-clonic seizures, also when NMDA-mediated neurotransmission is enhanced.
Letters to the Editor
- Biology
- 2000
Felbamate is the only marketed anticonvulsant agent with unequivocal NMDA receptor blocking activity at clinically relevant concentrations and Mazarati et al. are to be commended for highlighting the potential utility of felbamate and otherNMDA receptor antagonists in the termination of status epilepticus and for protecting against the associated seizure-induced brain damage.
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