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 Lettjournal_title
FEBS lettersauthors
Martin C,Ashley R,Shoshan-Barmatz Vdoi
10.1016/0014-5793(93)80969-2subject
Has Abstractpub_date
1993-08-09 00:00:00pages
77-81issue
1-2eissn
0014-5793issn
1873-3468pii
0014-5793(93)80969-2journal_volume
328pub_type
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