The interaction of local anesthetics with the ryanodine receptor of the sarcoplasmic reticulum

  title={The interaction of local anesthetics with the ryanodine receptor of the sarcoplasmic reticulum},
  author={Varda Shoshan-Barmatz and Sigalit Zchut},
  journal={The Journal of Membrane Biology},
SummaryThe effects of various local anesthetics (LAs) on the skeletal muscle ryanodine receptor were tested. The LAs were divided into three categories according to their effects on the binding of ryanodine to the junctional sarcoplasmic reticulum membranes. Ryanodine binding was assayed in the presence of 0.2 m NaCl and 10 μm CaCl2. Tetracaine and dibucaine inhibit the binding with half-maximal inhibition (CI50) of 0.12 and 0.25 mm, respectively, while inhibition by benzocaine and procaine… 
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Fast kinetic studies on the allosteric interactions between acetylcholine receptor and local anesthetic binding sites.
Preincubation of receptor-rich membrane fragments from Torpedo marmorata with tertiary amine local anesthetics and several toxins, modifies the amplitude and time course of the relaxation processes monitored upon rapid mixing of the membrane fragments with the fluorescent agonist, Dns-C6-Cho.
Action of local anesthetics on coupling systems in muscle.
  • C. Bianchi, T. Bolton
  • Biology, Chemistry
    The Journal of pharmacology and experimental therapeutics
  • 1967
It is proposed that the charged and uncharged forms of the local anesthetic act in a synergistic manner at the excitable surface membrane to block the action potential but act antagonistically at the membrane of the sarcoplasmic reticulum and the t-tubule with respect to excitation-contraction coupling in muscle.
ATP-dependent interaction of propranolol and local anaesthetic with sarcoplasmic reticulum. Stimulation of Ca2+ efflux.
The results suggest that propranolol and some local anaesthetics, in the presence of ATP, stimulate Ca2+ efflux by modifying a protein factor(s) rather than the phospholipid bilayer.
Local anesthetics: hydrophilic and hydrophobic pathways for the drug- receptor reaction
  • B. Hille
  • Biology
    The Journal of general physiology
  • 1977
The results are interpreted in terms of a single receptor in Na channels for the different drug types, and any drug form in the channel increases the probability of closing the inactivation gate which, in effect, is equivalent to a negative shift of the voltage dependence of inactivation.
Calcium-Binding Properties of Sarcoplasmic Reticulum As Influenced by ATP, Caffeine, Quinine, and Local Anesthetics
  • A. Carvalho
  • Biology
    The Journal of general physiology
  • 1968
The effects of caffeine, quinine, and of local anesthetics on the binding of Ca by the isolated reticulum are related to the effects of these agents on 45Ca fluxes and on the twitch output observed in whole muscles.
The displacement of membrane calcium by a local anesthetic (chlorpromazine).
The interaction of drugs with the sarcoplasmic reticulum.
The interaction of drugs with the sarcoplasmic reticulum membrane may provide structural models that are applicable to other biological membranes, as the overall structural properties of this membrane appear not to be unique.
Ryanodine binding to sarcoplasmic reticulum membrane; comparison between cardiac and skeletal muscle.