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

@article{citeulike:4726789, 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 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 occurs with CI50 of about 10-fold higher. Lidocaine, its analogue QX-314, and prilocaine, on the other hand, stimulate the binding up to fourfold with half-maximal stimulation occurring with about 2 mm of the drugs. Lidocaine increases both the receptor affinity for ryanodine by about fivefold and the rate of ryanodine association with its binding site by about 10-fold.}, author = {Shoshan-Barmatz, Varda and Zchut, Sigalit}, citeulike-article-id = {4726789}, citeulike-linkout-0 = {http://dx.doi.org/10.1007/BF00233797}, citeulike-linkout-1 = {http://www.springerlink.com/content/j235v4357787lu61}, doi = {10.1007/BF00233797}, journal = {Journal of Membrane Biology}, keywords = {receptor, reticulum, ryanodine, ryr, sarcoplasmic, tetracaine}, month = {January}, number = {2}, pages = {171--181}, posted-at = {2009-06-03 00:14:58}, priority = {2}, title = {The interaction of local anesthetics with the ryanodine receptor of the sarcoplasmic reticulum}, url = {http://dx.doi.org/10.1007/BF00233797}, volume = {133}, year = {1993} }

TY - JOUR ID - citeulike:4726789 L3 - citeulike-article-id:4726789 N2 - 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 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 occurs with CI50 of about 10-fold higher. Lidocaine, its analogue QX-314, and prilocaine, on the other hand, stimulate the binding up to fourfold with half-maximal stimulation occurring with about 2 mm of the drugs. Lidocaine increases both the receptor affinity for ryanodine by about fivefold and the rate of ryanodine association with its binding site by about 10-fold. IS - 2 JF - Journal of Membrane Biology EP - 181 TI - The interaction of local anesthetics with the ryanodine receptor of the sarcoplasmic reticulum VL - 133 SP - 171 KW - receptor KW - reticulum KW - ryanodine KW - ryr KW - sarcoplasmic KW - tetracaine AU - Shoshan-Barmatz, Varda AU - Zchut, Sigalit PY - 1993/01/01/ UR - http://dx.doi.org/10.1007/BF00233797 ER -