Matches in SemOpenAlex for { <https://semopenalex.org/work/W4239265319> ?p ?o ?g. }
Showing items 1 to 83 of
83
with 100 items per page.
- W4239265319 endingPage "889" @default.
- W4239265319 startingPage "885" @default.
- W4239265319 abstract "Local anesthetics suppress excitability by interfering with ion channel function.Ensheathment of peripheral nerve fibers, however, impedes diffusion of drugs to the ion channels and may influence the evaluation of local anesthetic potencies. Investigating ion channels in excised membrane patches avoids these diffusion barriers. We investigated the effect of local anesthetics with voltage-dependent Na+ and K+ channels in enzymatically dissociated sciatic nerve fibers of Xenopus laevis using the patch clamp method. The outside-out configuration was chosen to apply drugs to the external face of the membrane. Local anesthetics reversibly blocked the transient Na+ inward current, as well as the steady-state K+ outward current. Half-maximal tonic inhibiting concentrations (IC50), as obtained from concentration-effect curves for Na+ current block were: tetracaine 0.7 [micro sign]M, etidocaine 18 [micro sign]M, bupivacaine 27 [micro sign]M, procaine 60 [micro sign]M, mepivacaine 149 [micro sign]M, and lidocaine 204 [micro sign]M. The values for voltage-dependent K+ current block were: bupivacaine 92 [micro sign]M, etidocaine 176 [micro sign]M, tetracaine 946 [micro sign]M, lidocaine 1118 [micro sign]M, mepivacaine 2305 [micro sign]M, and procaine 6302 [micro sign]M. Correlation of potencies with octanol:buffer partition coefficients (logP0) revealed that ester-bound local anesthetics were more potent in blocking Na+ channels than amide drugs. Within these groups, lipophilicity governed local anesthetic potency. We conclude that local anesthetic action on peripheral nerve ion channels is mediated via lipophilic drug-channel interactions. Implications: Half-maximal blocking concentrations of commonly used local anesthetics for Na+ and K+ channel block were determined on small membrane patches of peripheral nerve fibers. Because drugs can directly diffuse to the ion channel in this model, these data result from direct interactions of the drugs with ion channels. (Anesth Analg 1998;87:885-9)" @default.
- W4239265319 created "2022-05-12" @default.
- W4239265319 creator A5036218939 @default.
- W4239265319 creator A5056104266 @default.
- W4239265319 creator A5058372752 @default.
- W4239265319 date "1998-10-01" @default.
- W4239265319 modified "2023-10-18" @default.
- W4239265319 title "Fundamental Properties of Local Anesthetics" @default.
- W4239265319 cites W1965878712 @default.
- W4239265319 cites W1967175787 @default.
- W4239265319 cites W1991096622 @default.
- W4239265319 cites W1993584057 @default.
- W4239265319 cites W1999858837 @default.
- W4239265319 cites W2009667219 @default.
- W4239265319 cites W2057232083 @default.
- W4239265319 cites W2069884282 @default.
- W4239265319 cites W2072749656 @default.
- W4239265319 cites W2074840709 @default.
- W4239265319 cites W2106140308 @default.
- W4239265319 cites W2116411564 @default.
- W4239265319 cites W2126997063 @default.
- W4239265319 cites W2279980834 @default.
- W4239265319 doi "https://doi.org/10.1213/00000539-199810000-00026" @default.
- W4239265319 hasPublicationYear "1998" @default.
- W4239265319 type Work @default.
- W4239265319 citedByCount "16" @default.
- W4239265319 countsByYear W42392653192012 @default.
- W4239265319 countsByYear W42392653192015 @default.
- W4239265319 countsByYear W42392653192021 @default.
- W4239265319 crossrefType "journal-article" @default.
- W4239265319 hasAuthorship W4239265319A5036218939 @default.
- W4239265319 hasAuthorship W4239265319A5056104266 @default.
- W4239265319 hasAuthorship W4239265319A5058372752 @default.
- W4239265319 hasBestOaLocation W42392653191 @default.
- W4239265319 hasConcept C12554922 @default.
- W4239265319 hasConcept C170493617 @default.
- W4239265319 hasConcept C185592680 @default.
- W4239265319 hasConcept C2778162923 @default.
- W4239265319 hasConcept C2778455913 @default.
- W4239265319 hasConcept C2778994108 @default.
- W4239265319 hasConcept C2779429755 @default.
- W4239265319 hasConcept C2779828710 @default.
- W4239265319 hasConcept C2780149897 @default.
- W4239265319 hasConcept C42219234 @default.
- W4239265319 hasConcept C50254741 @default.
- W4239265319 hasConcept C55493867 @default.
- W4239265319 hasConcept C71924100 @default.
- W4239265319 hasConcept C86803240 @default.
- W4239265319 hasConceptScore W4239265319C12554922 @default.
- W4239265319 hasConceptScore W4239265319C170493617 @default.
- W4239265319 hasConceptScore W4239265319C185592680 @default.
- W4239265319 hasConceptScore W4239265319C2778162923 @default.
- W4239265319 hasConceptScore W4239265319C2778455913 @default.
- W4239265319 hasConceptScore W4239265319C2778994108 @default.
- W4239265319 hasConceptScore W4239265319C2779429755 @default.
- W4239265319 hasConceptScore W4239265319C2779828710 @default.
- W4239265319 hasConceptScore W4239265319C2780149897 @default.
- W4239265319 hasConceptScore W4239265319C42219234 @default.
- W4239265319 hasConceptScore W4239265319C50254741 @default.
- W4239265319 hasConceptScore W4239265319C55493867 @default.
- W4239265319 hasConceptScore W4239265319C71924100 @default.
- W4239265319 hasConceptScore W4239265319C86803240 @default.
- W4239265319 hasIssue "4" @default.
- W4239265319 hasLocation W42392653191 @default.
- W4239265319 hasLocation W42392653192 @default.
- W4239265319 hasOpenAccess W4239265319 @default.
- W4239265319 hasPrimaryLocation W42392653191 @default.
- W4239265319 hasRelatedWork W1987853217 @default.
- W4239265319 hasRelatedWork W1997132769 @default.
- W4239265319 hasRelatedWork W2041215106 @default.
- W4239265319 hasRelatedWork W2125734824 @default.
- W4239265319 hasRelatedWork W2329323248 @default.
- W4239265319 hasRelatedWork W2404135964 @default.
- W4239265319 hasRelatedWork W27014100 @default.
- W4239265319 hasRelatedWork W2980592086 @default.
- W4239265319 hasRelatedWork W4200412177 @default.
- W4239265319 hasRelatedWork W2181884568 @default.
- W4239265319 hasVolume "87" @default.
- W4239265319 isParatext "false" @default.
- W4239265319 isRetracted "false" @default.
- W4239265319 workType "article" @default.