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Pathway Description
Felbamate NMDA Antagonist Action Pathway
Homo sapiens
Drug Action Pathway
Felbamate is an anticonvulsant used to treat severe epilepsy, particularly in adults.
The mechanism by which Felbamate exerts its anticonvulsant activity is unknown, but in animal tests felbamate has properties in common with other marketed anticonvulsants. In vitro studies have found that it may be an antagonist at the strychnine-insensitive glycine-recognition site of the N-methyl-D-aspartate(NMDA) receptor-ionophore complex. This antagonism of the NMDA receptor blocks the glutamate from activating the receptor and prevents calcium from entering the neuron. This causes hyperpolarization of the neuron which increases the threshold for neuron activation, increasing the seizure threshold and decreasing seizure spread. It has also been indicated that Felbamate has inhibitory actions on GABA receptors and benzodiazepine receptors.
References
Felbamate NMDA Antagonist Pathway References
Leppik IE, Dreifuss FE, Pledger GW, Graves NM, Santilli N, Drury I, Tsay JY, Jacobs MP, Bertram E, Cereghino JJ, et al.: Felbamate for partial seizures: results of a controlled clinical trial. Neurology. 1991 Nov;41(11):1785-9. doi: 10.1212/wnl.41.11.1785.
Pubmed: 1944909
Kleckner NW, Glazewski JC, Chen CC, Moscrip TD: Subtype-selective antagonism of N-methyl-D-aspartate receptors by felbamate: insights into the mechanism of action. J Pharmacol Exp Ther. 1999 May;289(2):886-94.
Pubmed: 10215667
Harty TP, Rogawski MA: Felbamate block of recombinant N-methyl-D-aspartate receptors: selectivity for the NR2B subunit. Epilepsy Res. 2000 Mar;39(1):47-55. doi: 10.1016/s0920-1211(99)00108-4.
Pubmed: 10690753
Chang HR, Kuo CC: Molecular determinants of the anticonvulsant felbamate binding site in the N-methyl-D-aspartate receptor. J Med Chem. 2008 Mar 27;51(6):1534-45. doi: 10.1021/jm0706618. Epub 2008 Feb 27.
Pubmed: 18311896
Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M: DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. doi: 10.1093/nar/gkx1037.
Pubmed: 29126136
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