1993
DOI: 10.1007/bf00233797
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The interaction of local anesthetics with the ryanodine receptor of the sarcoplasmic reticulum

Abstract: The 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 microM 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 occurs with CI50 of ab… Show more

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Cited by 38 publications
(32 citation statements)
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“…The imidazopyridine derivative, sulmazole, increases the duration and frequency of RyR2 openings. Whereas the EC 50 for RyR2 activation by caffeine is between 0.2-1 millimolar, sulmazole displays much greater potency (400 µmol ) [24,25] . Digitalis glycosides Digoxin is one of the cardiac glycosides, a closely-related group of drugs that have in common specific effects on the myocardium.…”
Section: Ryr2 Agonistsmentioning
confidence: 99%
See 1 more Smart Citation
“…The imidazopyridine derivative, sulmazole, increases the duration and frequency of RyR2 openings. Whereas the EC 50 for RyR2 activation by caffeine is between 0.2-1 millimolar, sulmazole displays much greater potency (400 µmol ) [24,25] . Digitalis glycosides Digoxin is one of the cardiac glycosides, a closely-related group of drugs that have in common specific effects on the myocardium.…”
Section: Ryr2 Agonistsmentioning
confidence: 99%
“…These include both tertiary amines (eg procaine, tetracaine, and lidocaine), as well as quaternary amines (eg QX572 and QX314) [50] . Although procaine and tetracaine ( Figure 1C) are both effective at low millimolar concentrations, procaine appears to be more selective for RyR2 compared to RyR1.…”
Section: Ryr2 Antagonistsmentioning
confidence: 99%
“…In addition to their actions on voltage-activated ion channels, LA are also known to block some ligandactivated ion currents, including those activated by both types of mammalian acetylcholine (ACh) receptors [2], the Torpedo electric organ nicotinic receptor [3], and the mammalian ryanodine receptor in skeletal muscle [4]. Currents through second-messenger-activated ion channels coupled to heterotrimeric G-protein-linked receptors can also be inhibited by LA, as was demonstrated for the muscarinic ACh receptor [5].…”
Section: Introductionmentioning
confidence: 99%
“…Local anesthetics, and in particular procaine, have been described to reduce the caffeine-evoked calcium release from RyR type 2 in gerbil hippocampal neurons [31], but also from sarcoplasmic reticulum [32]. Because RyR plays a critical role in the regulation of calcium release from the endoplasmic reticulum in the brain, impairment of which is believed to contribute to the development of AD, the effect of ryanodine on the Aß 1-42 -induced neurotoxicity was tested on PC12 cells.…”
Section: Discussionmentioning
confidence: 99%