Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
8
pubmed:dateCreated
1996-6-18
pubmed:abstractText
The effects of free polyunsaturated fatty acids (PUFA) on the binding of ligands to receptors on voltage-sensitive Na+ channels of neonatal rat cardiac myocytes were assessed. The radioligand was [benzoyl-2,5-(3)H] batrachotoxinin A 20alpha-benzoate ([(3)H]BTXB), a toxin that binds to the Na+ channel. The PUFA that have been shown to be antiarrhythmic, including eicosapentaenoic acid (EPA; C20:5n-3), docosahexaenoic acid (DHA; C22:6n-3), eicosatetraynoic acid (ETYA), linolenic acid (C18:3n-3), and linoleic acid (C18:2n-6), inhibited [(3)H]BTXB binding in a dose-dependent fashion with IC50 values of 28-35 microM, whereas those fatty acids that have no antiarrhythmic effects including saturated fatty acid (stearic acid, C18:0), monounsaturated fatty acid (oleic acid; C18:1n-9), and EPA methyl ester did not have a significant effect on [(3)H]BTXB binding. Enrichment of the myocyte membrane with cholesterol neither affected [(3)H]BTXB binding when compared with control cells nor altered the inhibitory effects of PUFA on [(3)H]BTXB binding. Scatchard analysis of [(3)H]BTXB binding showed that EPA reduced the maximal binding without altering the Kd for [(3)H]BTXB binding, indicating allosteric inhibition. The inhibition by EPA of [(3)H]BTXB binding was reversible (within 30 min) when delipidated bovine serum albumin was added. The binding of the PUFA to this site on the Na+ channel is reversible and structure-specific and occurs at concentrations close to those required for apparent antiarrhythmic effects and a blocking effect on the Na+ current, suggesting that binding of the PUFA at this site relates to their antiarrhythmic action.
pubmed:grant
pubmed:commentsCorrections
http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-1321440, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-1371330, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-1551431, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-1662467, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-1775367, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-2119911, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-2240249, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-2443266, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-2459775, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-2468291, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-2471269, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-2559978, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-2727703, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-2728003, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-29897, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-3147335, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-6247957, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-6321944, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-7479925, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-7522322, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-7563024, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-7695617, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-7732020, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-7937911, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-8025371, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-8127910, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-8183925, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-8218171, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-8488555, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-8606532, http://linkedlifedata.com/resource/pubmed/commentcorrection/8622972-8851173
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0027-8424
pubmed:author
pubmed:issnType
Print
pubmed:day
16
pubmed:volume
93
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
3542-6
pubmed:dateRevised
2009-11-18
pubmed:meshHeading
pubmed:year
1996
pubmed:articleTitle
Evidence that free polyunsaturated fatty acids modify Na+ channels by directly binding to the channel proteins.
pubmed:affiliation
Department of Medicine, Harvard Medical School, Boston, MA 02114, USA.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S.