Matches in SemOpenAlex for { <https://semopenalex.org/work/W1992287708> ?p ?o ?g. }
Showing items 1 to 91 of
91
with 100 items per page.
- W1992287708 endingPage "995" @default.
- W1992287708 startingPage "986" @default.
- W1992287708 abstract "Anesthetics bound to model membranes were observed directly by means of deuterium nuclear magnetic resonance (NMR). The specifically deuterated local anesthetics procaine and tetracaine were synthesized, and their partition coefficients (water:phosphatidylcholine) and pKa values determined. The interaction of these anesthetics with lamellar dispersions of egg phosphatidylcholine was studied by 2H nuclear magnetic resonance and by electron spin resonance (ESR) of a spin-labelled phospholipid at low (5.5) and high (9.5) pH. The ESR experiments suggest that tetracaine intercalates in the membrane and that it equilibrates between water and the phospholipid bilayers of the multilamellar system. The NMR results are consistent with a model where the anesthetic is (1) free in water, (2) weakly bound, and (3) strongly bound to the membrane. A fast exchange exists between the two first sites, but exchange is slow with the third site. Binding of type 3 is observed only at high pH for procaine, whereas it is found both at low and high pH for tetracaine. Calculations of the partition coefficients for the charged and uncharged forms of tetracaine indicate that both sites, 2 and 3, are occupied by the charged form at low pH and by the uncharged form at high pH. The partition coefficient for the weakly bound species was estimated from an analysis of the dependence of line width on the lipid to water ratio. The NMR data suggest that the binding sites for the strongly bound charged and uncharged species are different, the former probably being closer to the membrane-water interface. Estimates of molecular order parameters for the strongly bound species indicate that it is located with its long molecular axis approximately parallel to the director for ordering of the fatty acyl chains. A small increase in lipid ordering by tetracaine is observed at low pH, as evidenced by 2H NMR of the deuterated N-methyl groups of phosphatidylcholine; the reverse occurs at high pH." @default.
- W1992287708 created "2016-06-24" @default.
- W1992287708 creator A5016723787 @default.
- W1992287708 creator A5054558058 @default.
- W1992287708 creator A5073900195 @default.
- W1992287708 creator A5076275635 @default.
- W1992287708 date "1980-10-01" @default.
- W1992287708 modified "2023-10-03" @default.
- W1992287708 title "Multiple binding sites for local anesthetics in membranes: characterization of the sites and their equilibria by deuterium NMR of specifically deuterated procaine and tetracaine" @default.
- W1992287708 doi "https://doi.org/10.1139/o80-134" @default.
- W1992287708 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/6257349" @default.
- W1992287708 hasPublicationYear "1980" @default.
- W1992287708 type Work @default.
- W1992287708 sameAs 1992287708 @default.
- W1992287708 citedByCount "101" @default.
- W1992287708 countsByYear W19922877082012 @default.
- W1992287708 countsByYear W19922877082015 @default.
- W1992287708 countsByYear W19922877082019 @default.
- W1992287708 countsByYear W19922877082020 @default.
- W1992287708 countsByYear W19922877082022 @default.
- W1992287708 crossrefType "journal-article" @default.
- W1992287708 hasAuthorship W1992287708A5016723787 @default.
- W1992287708 hasAuthorship W1992287708A5054558058 @default.
- W1992287708 hasAuthorship W1992287708A5073900195 @default.
- W1992287708 hasAuthorship W1992287708A5076275635 @default.
- W1992287708 hasConcept C121332964 @default.
- W1992287708 hasConcept C126061179 @default.
- W1992287708 hasConcept C178790620 @default.
- W1992287708 hasConcept C185592680 @default.
- W1992287708 hasConcept C192552737 @default.
- W1992287708 hasConcept C2776330855 @default.
- W1992287708 hasConcept C2778455913 @default.
- W1992287708 hasConcept C2778918659 @default.
- W1992287708 hasConcept C2779828710 @default.
- W1992287708 hasConcept C2780149897 @default.
- W1992287708 hasConcept C32909587 @default.
- W1992287708 hasConcept C41625074 @default.
- W1992287708 hasConcept C42219234 @default.
- W1992287708 hasConcept C43617362 @default.
- W1992287708 hasConcept C55493867 @default.
- W1992287708 hasConcept C58364064 @default.
- W1992287708 hasConcept C62520636 @default.
- W1992287708 hasConcept C66974803 @default.
- W1992287708 hasConcept C71240020 @default.
- W1992287708 hasConcept C71924100 @default.
- W1992287708 hasConcept C73673656 @default.
- W1992287708 hasConcept C8010536 @default.
- W1992287708 hasConceptScore W1992287708C121332964 @default.
- W1992287708 hasConceptScore W1992287708C126061179 @default.
- W1992287708 hasConceptScore W1992287708C178790620 @default.
- W1992287708 hasConceptScore W1992287708C185592680 @default.
- W1992287708 hasConceptScore W1992287708C192552737 @default.
- W1992287708 hasConceptScore W1992287708C2776330855 @default.
- W1992287708 hasConceptScore W1992287708C2778455913 @default.
- W1992287708 hasConceptScore W1992287708C2778918659 @default.
- W1992287708 hasConceptScore W1992287708C2779828710 @default.
- W1992287708 hasConceptScore W1992287708C2780149897 @default.
- W1992287708 hasConceptScore W1992287708C32909587 @default.
- W1992287708 hasConceptScore W1992287708C41625074 @default.
- W1992287708 hasConceptScore W1992287708C42219234 @default.
- W1992287708 hasConceptScore W1992287708C43617362 @default.
- W1992287708 hasConceptScore W1992287708C55493867 @default.
- W1992287708 hasConceptScore W1992287708C58364064 @default.
- W1992287708 hasConceptScore W1992287708C62520636 @default.
- W1992287708 hasConceptScore W1992287708C66974803 @default.
- W1992287708 hasConceptScore W1992287708C71240020 @default.
- W1992287708 hasConceptScore W1992287708C71924100 @default.
- W1992287708 hasConceptScore W1992287708C73673656 @default.
- W1992287708 hasConceptScore W1992287708C8010536 @default.
- W1992287708 hasIssue "10" @default.
- W1992287708 hasLocation W19922877081 @default.
- W1992287708 hasLocation W19922877082 @default.
- W1992287708 hasOpenAccess W1992287708 @default.
- W1992287708 hasPrimaryLocation W19922877081 @default.
- W1992287708 hasRelatedWork W1971836911 @default.
- W1992287708 hasRelatedWork W2004975012 @default.
- W1992287708 hasRelatedWork W2009240753 @default.
- W1992287708 hasRelatedWork W2009484394 @default.
- W1992287708 hasRelatedWork W2015713265 @default.
- W1992287708 hasRelatedWork W2036020781 @default.
- W1992287708 hasRelatedWork W2045179772 @default.
- W1992287708 hasRelatedWork W2107641298 @default.
- W1992287708 hasRelatedWork W4238604091 @default.
- W1992287708 hasRelatedWork W77534462 @default.
- W1992287708 hasVolume "58" @default.
- W1992287708 isParatext "false" @default.
- W1992287708 isRetracted "false" @default.
- W1992287708 magId "1992287708" @default.
- W1992287708 workType "article" @default.