The effect of local anaesthetics on the ryanodine receptor/Ca2+ release channel of brain microsomal membranes

Cecile Martin, Richard Ashley, Varda Shoshan-Barmatz

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22 Scopus citations

Abstract

The effects of various local anaesthetics (LAs) on ryanodine binding of the sheep brain ryanodine receptor were tested. Tetracaine and dibucaine inhibit the binding with half-maximal inhibition (CI50) of 0.12 mM and 0.7 mM, respectively. Lidocaine and its analog QX-314, on the other hand, stimulate the binding up to 3-fold with half-maximal stimulation occurring with about 2 mM of the drugs. Lidocaine increases both the receptor affinity for ryanodine by about 5-fold and the rate of ryanodine association with its binding site by about 6-fold. Tetracaine and lidocaine also interact with the purified brain ryanodine receptor and produce inhibitory and stimulatory effects similar to those obtained with the membranebound receptor. The interaction of the LAs with the brain ryanodine receptor, as well as with the skeletal muscle receptor [J. Memb. Biol. 133 (1993) 171-182], suggest that ryanodine receptor possesses intrinsic binding site(s) for LAs.

Original languageEnglish
Pages (from-to)77-81
Number of pages5
JournalFEBS Letters
Volume328
Issue number1-2
DOIs
StatePublished - 9 Aug 1993

Keywords

  • Brain microsome
  • Ca release channel
  • Local anaesthetic
  • Ryanodine receptor

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