High affinity for the rat brain sodium channel of newly discovered hydroxybenzoate saxitoxin analogues from the dinoflagellate Gymnodinium catenatum

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DOIResolve DOI: http://doi.org/10.1016/j.toxicon.2003.10.016
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TypeArticle
Journal titleToxicon
Volume43
Issue1
Pages101104; # of pages: 4
Subjectsaxitoxin; sodium channel; paralytic shellfish poison; gymnodinium catenatum; hydroxybenzoate
AbstractThe paralytic shellfish poison family has been recently extended by the discovery of several analogues possessing a hydoxybenzoate moiety instead of the carbamoyl group one finds in saxitoxin, the parent molecule of this toxin family. We have investigated the potency of these new analogues on a representative isoform of the pharmacological target of these toxins, the voltage gated sodium channel. These toxins were found to have KI's in the low nanomolar range, only slightly less potent than saxitoxin. The hydroxybenzoate group may increase the lipophilicity of these toxins and improve their ability to pass through epithelia and therefore its uptake and elimination in both intoxication victims and animals that bioaccumulate paralytic shellfish toxins.
Publication date
PublisherElsevier
Copyright noticeCopyright 2003 Elsevier Ltd. All rights reserved.
LanguageEnglish
AffiliationNRC Institute for Marine Biosciences; National Research Council Canada; Measurement Science and Standards
Peer reviewedYes
NRC number1372
NPARC number3538514
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Record identifierfa42dff1-5176-402b-a1bf-ff9c12628fea
Record created2009-03-01
Record modified2016-05-09
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