Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5050
DC FieldValueLanguage
dc.contributor.authorFusi, Fabioen_us
dc.contributor.authorIozzi, D.en_us
dc.contributor.authorSgaragli, GIAN PIETROen_us
dc.contributor.authorFrosini, Mariaen_us
dc.date.accessioned2021-03-30T15:48:40Z-
dc.date.available2021-03-30T15:48:40Z-
dc.date.issued2005-
dc.identifier.issn0006-2952en_US
dc.identifier.urihttp://hdl.handle.net/20.500.12779/5050-
dc.description36339en_US
dc.description.abstractIn the present study, the effects of 3,5-di-t-butylcatechol (DTCAT) on ryanodine receptor Ca(2+) channel (RyRC) of skeletal muscle sarcoplasmic reticulum (SR) vesicles were investigated, both by monitoring extravesicular Ca(2+) concentration directly with the Ca(2+) indicator dye arsenazo III and by studying the high-affinity [(3)H]ryanodine binding. DTCAT stimulated Ca(2+) release from junctional (terminal cisternae) vesicles in a concentration-dependent manner, with a threshold activating concentration of 30 microM and a pEC(50) value of 3.43+/-0.03 M. The release of Ca(2+) induced by DTCAT was antagonized in a concentration-dependent manner by ruthenium red, thus indicating that RyRC is involved in the mechanism of stimulation. A structure-activity relationship analysis carried out on a limited number of compounds suggested that both hydroxy and t-butyl groups in DTCAT were important for the activation of RyRC. DTCAT inhibited [(3)H]ryanodine binding to SR vesicles with a K(i) of 232.5 microM, thus indicating that it acted directly at the skeletal muscle ryanodine receptor binding site to stimulate Ca(2+) release. In conclusion, the ability of DTCAT to release Ca(2+) from TC vesicles of skeletal muscle is noteworthy in view of its possible use as an alternative compound to either caffeine or halothane for performing the "In vitro contracture test" to diagnose the susceptibility of some patients to develop malignant hyperthermia under particular pharmacological treatments.en_US
dc.language.isoenen_US
dc.relationNoneen_US
dc.relation.ispartofBIOCHEMICAL PHARMACOLOGYen_US
dc.title3,5-di-t-butylcatechol (DTCAT) as an activator of rat skeletal muscle ryanodine receptor Ca2+ channel (RyRC).en_US
dc.typeArticleen_US
dc.identifier.doi10.1016/j.bcp.2004.10.013en_US
dc.identifier.pmid15652239en_US
dc.identifier.scopus2-s2.0-11844304126en_US
dc.identifier.isiWOS:000226699800012en_US
dc.relation.volume69(3)en_US
dc.relation.issue3en_US
dc.description.firstpage485en_US
dc.description.lastpage491en_US
dc.description.thirdmissionNot applicableen_US
item.cerifentitytypePublications-
item.grantfulltextnone-
item.languageiso639-1en-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.openairetypeArticle-
item.fulltextNo Fulltext-
crisitem.author.orcid0000-0002-5737-8309-
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