FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2010302247> ?p ?o ?g. }

• W2010302247 endingPage "120" @default.
• W2010302247 startingPage "110" @default.
• W2010302247 abstract "Opioids enhance and prolong analgesia when applied as adjuvants to local anaesthetics (LAs). A possible molecular mechanism for this property is a direct inhibition of voltage-gated Na(+) channels which was reported for some opioids. Methadone is an effective adjuvant to LA and was recently reported to inhibit cardiac Na(+) channels. Here, we explore and compare LA properties of methadone and bupivacaine on neuronal Na(+) channels, excitability of peripheral nerves, and cell viability.Effects of methadone were explored on compound action potentials (CAP) of isolated mouse saphenous nerves. Patch clamp recordings were performed on Na(+) channels in ND7/23 cells, the α-subunits Nav1.2, Nav1.3, Nav1.7, and Nav1.8, and the hyperpolarization-activated cyclic nucleotide-gated channel 2 (HCN2). Cytotoxicity was determined using flow cytometry.Methadone (IC50 86-119 µM) is a state-dependent and unselective blocker on Nav1.2, Nav1.3, Nav1.7, and Nav1.8 with a potency comparable with that of bupivacaine (IC50 177 µM). Both bupivacaine and methadone also inhibit C- and A-fibre CAPs in saphenous nerves in a concentration-dependent manner. Tonic block of Nav1.7 revealed a discrete stereo-selectivity with a higher potency for levomethadone than for dextromethadone. Methadone is also a weak blocker of HCN2 channels. Both methadone and bupivacaine induce a pronounced cytotoxicity at concentrations required for LA effects.Methadone induces typical LA effects by inhibiting Na(+) channels with a potency similar to that of bupivacaine. This hitherto unknown property of methadone might contribute to its high efficacy when applied as an adjuvant to LA." @default.
• W2010302247 created "2016-06-24" @default.
• W2010302247 creator A5002308035 @default.
• W2010302247 creator A5012209580 @default.
• W2010302247 creator A5041082258 @default.
• W2010302247 creator A5048398717 @default.
• W2010302247 creator A5051804264 @default.
• W2010302247 creator A5065559249 @default.
• W2010302247 creator A5070551383 @default.
• W2010302247 creator A5070885724 @default.
• W2010302247 creator A5086898119 @default.
• W2010302247 creator A5089961229 @default.
• W2010302247 date "2015-01-01" @default.
• W2010302247 modified "2023-10-16" @default.
• W2010302247 title "Methadone is a local anaesthetic-like inhibitor of neuronal Na + channels and blocks excitability of mouse peripheral nerves" @default.
• W2010302247 cites W1555971153 @default.
• W2010302247 cites W1993462384 @default.
• W2010302247 cites W1994011917 @default.
• W2010302247 cites W1996658533 @default.
• W2010302247 cites W1997976993 @default.
• W2010302247 cites W2001847376 @default.
• W2010302247 cites W2004681085 @default.
• W2010302247 cites W2008962464 @default.
• W2010302247 cites W2016634006 @default.
• W2010302247 cites W2018596562 @default.
• W2010302247 cites W2021724151 @default.
• W2010302247 cites W2033809002 @default.
• W2010302247 cites W2037989588 @default.
• W2010302247 cites W2040173329 @default.
• W2010302247 cites W2045234204 @default.
• W2010302247 cites W2049587168 @default.
• W2010302247 cites W2056275026 @default.
• W2010302247 cites W2059688417 @default.
• W2010302247 cites W2060972591 @default.
• W2010302247 cites W2061414979 @default.
• W2010302247 cites W2065983435 @default.
• W2010302247 cites W2076550065 @default.
• W2010302247 cites W2078840491 @default.
• W2010302247 cites W2092732744 @default.
• W2010302247 cites W2095679461 @default.
• W2010302247 cites W2119663072 @default.
• W2010302247 cites W2124798906 @default.
• W2010302247 cites W2140003901 @default.
• W2010302247 cites W2142419903 @default.
• W2010302247 cites W2142828467 @default.
• W2010302247 cites W2151756831 @default.
• W2010302247 cites W2151899782 @default.
• W2010302247 cites W2159636951 @default.
• W2010302247 cites W2162704927 @default.
• W2010302247 cites W2322065048 @default.
• W2010302247 cites W2330671935 @default.
• W2010302247 cites W3021398226 @default.
• W2010302247 doi "https://doi.org/10.1093/bja/aeu206" @default.
• W2010302247 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/25012584" @default.
• W2010302247 hasPublicationYear "2015" @default.
• W2010302247 type Work @default.
• W2010302247 sameAs 2010302247 @default.
• W2010302247 citedByCount "24" @default.
• W2010302247 countsByYear W20103022472014 @default.
• W2010302247 countsByYear W20103022472015 @default.
• W2010302247 countsByYear W20103022472016 @default.
• W2010302247 countsByYear W20103022472017 @default.
• W2010302247 countsByYear W20103022472018 @default.
• W2010302247 countsByYear W20103022472019 @default.
• W2010302247 countsByYear W20103022472020 @default.
• W2010302247 countsByYear W20103022472022 @default.
• W2010302247 countsByYear W20103022472023 @default.
• W2010302247 crossrefType "journal-article" @default.
• W2010302247 hasAuthorship W2010302247A5002308035 @default.
• W2010302247 hasAuthorship W2010302247A5012209580 @default.
• W2010302247 hasAuthorship W2010302247A5041082258 @default.
• W2010302247 hasAuthorship W2010302247A5048398717 @default.
• W2010302247 hasAuthorship W2010302247A5051804264 @default.
• W2010302247 hasAuthorship W2010302247A5065559249 @default.
• W2010302247 hasAuthorship W2010302247A5070551383 @default.
• W2010302247 hasAuthorship W2010302247A5070885724 @default.
• W2010302247 hasAuthorship W2010302247A5086898119 @default.
• W2010302247 hasAuthorship W2010302247A5089961229 @default.
• W2010302247 hasBestOaLocation W20103022471 @default.
• W2010302247 hasConcept C126322002 @default.
• W2010302247 hasConcept C131453863 @default.
• W2010302247 hasConcept C147944092 @default.
• W2010302247 hasConcept C170493617 @default.
• W2010302247 hasConcept C185263204 @default.
• W2010302247 hasConcept C185592680 @default.
• W2010302247 hasConcept C202751555 @default.
• W2010302247 hasConcept C2777752497 @default.
• W2010302247 hasConcept C2778767360 @default.
• W2010302247 hasConcept C2781063702 @default.
• W2010302247 hasConcept C2781328992 @default.
• W2010302247 hasConcept C42219234 @default.
• W2010302247 hasConcept C55493867 @default.
• W2010302247 hasConcept C57992300 @default.
• W2010302247 hasConcept C66974803 @default.
• W2010302247 hasConcept C71240020 @default.
• W2010302247 hasConcept C71924100 @default.
• W2010302247 hasConcept C98274493 @default.
• W2010302247 hasConceptScore W2010302247C126322002 @default.

• next