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• W2083516189 endingPage "40" @default.
• W2083516189 startingPage "31" @default.
• W2083516189 abstract "The aim of the present study was to determine the effects of 4-chloro-m-cresol (4-CmC), a preservative often added to drugs intravenously administered, on the skeletal muscle sarcoplasmic reticulum (SR) Ca2+ release channel/ryanodine receptor. In heavy SR vesicles obtained from rabbit back muscles, 4-CmC stimulated (Ca2+)-activated [3H]ryanodine binding with an EC50 of about 100 microM. In the same concentration range, 4-CmC directly activated the isolated Ca2+ release channel reconstituted into planar lipid bilayers. The sensitivity to 4-CmC was found to be higher when applied to the luminal side of the channel suggesting binding site(s) different from those of nucleotides and caffeine. In skeletal muscle fibre bundles obtained from biopsies of patients susceptible to malignant hyperthermia, a skeletal muscle disease caused by point mutations in the ryanodine receptor, 4-CmC evoked caffeine-like contractures. Contrary to caffeine which induces contractures in millimolar concentrations, the threshold concentration for 4-CmC was 25 microM compared to 75 microM for non-mutated control fibres. Since these data strongly indicate that 4-CmC specifically activates SR Ca2+ release also in intact cell systems, this substance might become a powerful tool to investigate ryanodine receptor-mediated Ca2+ release in muscle and non-muscle tissue." @default.
• W2083516189 created "2016-06-24" @default.
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• W2083516189 date "1996-02-01" @default.
• W2083516189 modified "2023-09-26" @default.
• W2083516189 title "4-chloro- m -cresol, a potent and specific activator of the skeletal muscle ryanodine receptor" @default.
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• W2083516189 doi "https://doi.org/10.1016/0304-4165(95)00131-x" @default.
• W2083516189 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/8605229" @default.
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