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

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 membrane-bound 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.

journal_name

FEBS Lett

journal_title

FEBS letters

authors

Martin C,Ashley R,Shoshan-Barmatz V

doi

10.1016/0014-5793(93)80969-2

subject

Has Abstract

pub_date

1993-08-09 00:00:00

pages

77-81

issue

1-2

eissn

0014-5793

issn

1873-3468

pii

0014-5793(93)80969-2

journal_volume

328

pub_type

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