FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2035587250> ?p ?o ?g. }

• W2035587250 endingPage "1992" @default.
• W2035587250 startingPage "1981" @default.
• W2035587250 abstract "Felbamate (FBM) is a potent nonsedative anticonvulsant whose clinical effect is chiefly related to gating modification (and thus use-dependent inhibition) rather than pore block of N-methyl-D-aspartate (NMDA) channels at pH 7.4. Using whole-cell recording in rat hippocampal neurons, we examined the effect of extracellular pH on FBM action. In sharp contrast to the findings at pH 7.4, the inhibitory effect of FBM on NMDA currents shows much weakened use-dependence at pH 8.4. Moreover, FBM neither accelerates the activation kinetics of the NMDA channel, nor enhances the currents elicited by very low concentrations of NMDA at pH 8.4. These differential effects of FBM between pH 7.4 and 8.4 are abolished in the mutant NMDA channels which lack proton sensitivity. Most interestingly, the inhibitory effect of FBM becomes flow-dependent and is evidently stronger in inward than in outward NMDA currents at pH 8.4. These findings indicate that FBM has a significantly more manifest pore-blocking effect on the NMDA channel at pH 8.4 than at pH 7.4. 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. Also, we find that the inhibitory effect of FBM on NMDA currents is antagonized by external but not internal Na+, and that increase of external Na+ decreases the binding rate without altering the unbinding rate of FBM. These findings indicate that the FBM binding site faces the extracellular rather than the intracellular solution, and coincides with the outmost ionic (e.g., Na+) site in the NMDA channel pore. We conclude that the FBM binding site very likely is located in the external pore mouth, where extracellular proton, Na+, FBM, and NMDA channel gating have an orchestrating effect." @default.
• W2035587250 created "2016-06-24" @default.
• W2035587250 creator A5081521557 @default.
• W2035587250 creator A5084041495 @default.
• W2035587250 date "2007-09-01" @default.
• W2035587250 modified "2023-09-30" @default.
• W2035587250 title "Extracellular Proton-Modulated Pore-Blocking Effect of the Anticonvulsant Felbamate on NMDA Channels" @default.
• W2035587250 cites W110640999 @default.
• W2035587250 cites W1499205986 @default.
• W2035587250 cites W1594006457 @default.
• W2035587250 cites W1947219617 @default.
• W2035587250 cites W1957753057 @default.
• W2035587250 cites W1967932180 @default.
• W2035587250 cites W1984804294 @default.
• W2035587250 cites W1987398739 @default.
• W2035587250 cites W1987949200 @default.
• W2035587250 cites W1995396359 @default.
• W2035587250 cites W1996299779 @default.
• W2035587250 cites W2003636640 @default.
• W2035587250 cites W2016550668 @default.
• W2035587250 cites W2019357760 @default.
• W2035587250 cites W2034961929 @default.
• W2035587250 cites W2038250290 @default.
• W2035587250 cites W2048011585 @default.
• W2035587250 cites W2050037509 @default.
• W2035587250 cites W2055381303 @default.
• W2035587250 cites W2056422818 @default.
• W2035587250 cites W2059334396 @default.
• W2035587250 cites W2059401172 @default.
• W2035587250 cites W2065169750 @default.
• W2035587250 cites W2065441702 @default.
• W2035587250 cites W2071529758 @default.
• W2035587250 cites W2088328293 @default.
• W2035587250 cites W2107438925 @default.
• W2035587250 cites W2107630141 @default.
• W2035587250 cites W2115248525 @default.
• W2035587250 cites W2116635659 @default.
• W2035587250 cites W2117745130 @default.
• W2035587250 cites W2127637463 @default.
• W2035587250 cites W2132358083 @default.
• W2035587250 cites W2147119933 @default.
• W2035587250 cites W2150400736 @default.
• W2035587250 cites W2154525124 @default.
• W2035587250 cites W4319308579 @default.
• W2035587250 cites W80467188 @default.
• W2035587250 doi "https://doi.org/10.1529/biophysj.106.103176" @default.
• W2035587250 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/1959524" @default.
• W2035587250 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/17513365" @default.
• W2035587250 hasPublicationYear "2007" @default.
• W2035587250 type Work @default.
• W2035587250 sameAs 2035587250 @default.
• W2035587250 citedByCount "8" @default.
• W2035587250 countsByYear W20355872502013 @default.
• W2035587250 crossrefType "journal-article" @default.
• W2035587250 hasAuthorship W2035587250A5081521557 @default.
• W2035587250 hasAuthorship W2035587250A5084041495 @default.
• W2035587250 hasBestOaLocation W20355872501 @default.
• W2035587250 hasConcept C12554922 @default.
• W2035587250 hasConcept C153461711 @default.
• W2035587250 hasConcept C169760540 @default.
• W2035587250 hasConcept C170493617 @default.
• W2035587250 hasConcept C17077164 @default.
• W2035587250 hasConcept C178790620 @default.
• W2035587250 hasConcept C185592680 @default.
• W2035587250 hasConcept C28406088 @default.
• W2035587250 hasConcept C519063684 @default.
• W2035587250 hasConcept C55493867 @default.
• W2035587250 hasConcept C67018056 @default.
• W2035587250 hasConcept C86803240 @default.
• W2035587250 hasConceptScore W2035587250C12554922 @default.
• W2035587250 hasConceptScore W2035587250C153461711 @default.
• W2035587250 hasConceptScore W2035587250C169760540 @default.
• W2035587250 hasConceptScore W2035587250C170493617 @default.
• W2035587250 hasConceptScore W2035587250C17077164 @default.
• W2035587250 hasConceptScore W2035587250C178790620 @default.
• W2035587250 hasConceptScore W2035587250C185592680 @default.
• W2035587250 hasConceptScore W2035587250C28406088 @default.
• W2035587250 hasConceptScore W2035587250C519063684 @default.
• W2035587250 hasConceptScore W2035587250C55493867 @default.
• W2035587250 hasConceptScore W2035587250C67018056 @default.
• W2035587250 hasConceptScore W2035587250C86803240 @default.
• W2035587250 hasIssue "6" @default.
• W2035587250 hasLocation W20355872501 @default.
• W2035587250 hasLocation W20355872502 @default.
• W2035587250 hasLocation W20355872503 @default.
• W2035587250 hasLocation W20355872504 @default.
• W2035587250 hasOpenAccess W2035587250 @default.
• W2035587250 hasPrimaryLocation W20355872501 @default.
• W2035587250 hasRelatedWork W1543054176 @default.
• W2035587250 hasRelatedWork W1991812693 @default.
• W2035587250 hasRelatedWork W2062396996 @default.
• W2035587250 hasRelatedWork W2067514449 @default.
• W2035587250 hasRelatedWork W2079519576 @default.
• W2035587250 hasRelatedWork W2081434191 @default.
• W2035587250 hasRelatedWork W2088328293 @default.
• W2035587250 hasRelatedWork W2132041019 @default.
• W2035587250 hasRelatedWork W2419336000 @default.
• W2035587250 hasRelatedWork W5653682 @default.

• next