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rdf:type | |
lifeskim:mentions | |
pubmed:dateCreated |
1991-6-27
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pubmed:abstractText |
Propionyl-L-carnitine (PC) protects perfused rat hearts against damage by ischemia-reperfusion. Activation of L-type calcium channel play a role on ischemia-reperfusion damage. Therefore, we studied the effect of PC on some properties of L-type calcium channels in an in vitro preparation from human myocardium sarcolemma (from patients with idiopathic dilated cardiomyopathy). Binding of the L-type calcium channel blockers isradipine [3H]-PN 200-110 (PN) to plasma membrane preparations revealed a single population of binding sites (total number: Bmax = 213 +/- 34 fM/mg protein and affinity: Kd = 152 +/- 19 nM; n = 6). The characteristics of these binding sites were evaluated in the presence and in the absence of Ca2+ and of calcium blockers (D-888, a verapamillike drug, and diltiazem). Incubation in a Ca2(+)-containing buffer increased the affinity of PN binding sites. Binding sites for PN were modulated by organic calcium channel blockers; in competition isotherms at 37 degrees C, D-888 (desmethoxyverapamil) decreased the PN binding, whereas diltiazem increased it. These results strongly suggest that the site labelled by PN is the voltage-operated calcium channel of the human myocardium. The addition of PC (1 mM) to plasma membranes labelled with PN at 37 degrees C decreased the affinity of the binding; this effect was counteracted by the addition of Ca2+ to the medium. This result was consistent with a competition between Ca2+ and PC. The effect of PC incubation at 4 degrees C was the opposite; at this temperature PC increased the affinity of the binding sites and the effect was obscured by Ca2+.(ABSTRACT TRUNCATED AT 250 WORDS)
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium Channel Blockers,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium Channels,
http://linkedlifedata.com/resource/pubmed/chemical/Carnitine,
http://linkedlifedata.com/resource/pubmed/chemical/Isradipine,
http://linkedlifedata.com/resource/pubmed/chemical/Oxadiazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Tritium,
http://linkedlifedata.com/resource/pubmed/chemical/propionylcarnitine
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0920-3206
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
5 Suppl 1
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
31-5
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:1851633-Binding Sites,
pubmed-meshheading:1851633-Calcium,
pubmed-meshheading:1851633-Calcium Channel Blockers,
pubmed-meshheading:1851633-Calcium Channels,
pubmed-meshheading:1851633-Carnitine,
pubmed-meshheading:1851633-Cell Membrane,
pubmed-meshheading:1851633-Culture Techniques,
pubmed-meshheading:1851633-Heart,
pubmed-meshheading:1851633-Humans,
pubmed-meshheading:1851633-Isradipine,
pubmed-meshheading:1851633-Myocardium,
pubmed-meshheading:1851633-Oxadiazoles,
pubmed-meshheading:1851633-Radioligand Assay,
pubmed-meshheading:1851633-Sarcolemma,
pubmed-meshheading:1851633-Tritium
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pubmed:year |
1991
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pubmed:articleTitle |
Effect of propionyl-L-carnitine on L-type calcium channels in human heart sarcolemma.
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pubmed:affiliation |
Servizio di Endocrinologia, Ospedale L. Sacco (Vialba), Milano, Italy.
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pubmed:publicationType |
Journal Article
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