| pubmed-article:17609421 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:17609421 | lifeskim:mentions | umls-concept:C0027882 | lld:lifeskim |
| pubmed-article:17609421 | lifeskim:mentions | umls-concept:C0007765 | lld:lifeskim |
| pubmed-article:17609421 | lifeskim:mentions | umls-concept:C0205145 | lld:lifeskim |
| pubmed-article:17609421 | lifeskim:mentions | umls-concept:C0010837 | lld:lifeskim |
| pubmed-article:17609421 | lifeskim:mentions | umls-concept:C0027934 | lld:lifeskim |
| pubmed-article:17609421 | lifeskim:mentions | umls-concept:C0037492 | lld:lifeskim |
| pubmed-article:17609421 | lifeskim:mentions | umls-concept:C0205245 | lld:lifeskim |
| pubmed-article:17609421 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
| pubmed-article:17609421 | lifeskim:mentions | umls-concept:C1551336 | lld:lifeskim |
| pubmed-article:17609421 | lifeskim:mentions | umls-concept:C1097445 | lld:lifeskim |
| pubmed-article:17609421 | pubmed:issue | 1 | lld:pubmed |
| pubmed-article:17609421 | pubmed:dateCreated | 2007-9-20 | lld:pubmed |
| pubmed-article:17609421 | pubmed:abstractText | The marine toxin gambierol, a polyether ladder toxin derived from the marine dinoflagellate Gambierdiscus toxicus, was evaluated for interaction with voltage-gated sodium channels (VGSCs) in cerebellar granule neuron (CGN) cultures. At concentrations ranging from 10 nM to 10 microM, gambierol alone had no effect on the intracellular Ca2+ concentration [Ca2+]i of exposed CGN cultures. Furthermore, there was no evidence of neurotoxicity in CGN cultures exposed for 2 h to gambierol (1 nM-10 microM). However, gambierol was a potent inhibitor (IC50 = 189 nM) of the elevation of [Ca2+]i that accompanies exposure of CGN cultures to the VGSC activator brevetoxin-2 (PbTx-2). To further explore the potential interaction of gambierol with VGSCs, the influence of gambierol on PbTx-2-induced neurotoxicity was assessed. Gambierol reduced the PbTx-2-induced efflux of lactate dehydrogenase in exposed CGN cultures in a concentration-dependent manner (IC50 = 471 nM). It is noteworthy that the potencies of gambierol as an inhibitor of both PbTx-2-induced Ca2+ influx and cytotoxicity were coincident. Finally, the inhibitory effects of gambierol on PbTx-2-induced elevation of [Ca2+]i were compared with those of brevenal, a natural inhibitor of the toxic effects of brevetoxin isolated from cultures of Karina brevis. Like gambierol, brevenal inhibited PbTx-2-induced elevation of [Ca2+]i in a concentration-dependent manner (IC50 = 108.6 nM). These results provide evidence for gambierol acting as a functional antagonist of neurotoxin site 5 on neuronal VGSCs. | lld:pubmed |
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| pubmed-article:17609421 | pubmed:language | eng | lld:pubmed |
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| pubmed-article:17609421 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:17609421 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:17609421 | pubmed:month | Oct | lld:pubmed |
| pubmed-article:17609421 | pubmed:issn | 0022-3565 | lld:pubmed |
| pubmed-article:17609421 | pubmed:author | pubmed-author:MurrayT FTF | lld:pubmed |
| pubmed-article:17609421 | pubmed:author | pubmed-author:BadenD GDG | lld:pubmed |
| pubmed-article:17609421 | pubmed:author | pubmed-author:LePageK TKT | lld:pubmed |
| pubmed-article:17609421 | pubmed:author | pubmed-author:RainierJ DJD | lld:pubmed |
| pubmed-article:17609421 | pubmed:author | pubmed-author:JohnsonH W... | lld:pubmed |
| pubmed-article:17609421 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:17609421 | pubmed:volume | 323 | lld:pubmed |
| pubmed-article:17609421 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:17609421 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:17609421 | pubmed:pagination | 174-9 | lld:pubmed |
| pubmed-article:17609421 | pubmed:dateRevised | 2011-11-17 | lld:pubmed |
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| pubmed-article:17609421 | pubmed:year | 2007 | lld:pubmed |
| pubmed-article:17609421 | pubmed:articleTitle | Gambierol acts as a functional antagonist of neurotoxin site 5 on voltage-gated sodium channels in cerebellar granule neurons. | lld:pubmed |
| pubmed-article:17609421 | pubmed:affiliation | Department of Biology, Xavier University of Louisiana, New Orleans, Louisiana, USA. | lld:pubmed |
| pubmed-article:17609421 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:17609421 | pubmed:publicationType | Research Support, N.I.H., Extramural | lld:pubmed |
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