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Brevetoxins, unique activators of voltage-sensitive sodium channels, bind to specific sites in rat brain synaptosomes.
Abstract
The polyether lipid-soluble toxins isolated from the marine dinoflagellate Ptychodiscus brevis (formerly Gymnodinium breve) have been determined to bind to a unique site associated with rat brain synaptosomes. Using [3H]brevetoxin PbTx-3 as a specific probe, binding was determined at 4 degrees in rat brain synaptosomes using a rapid centrifugation technique. Rosenthal analysis yields a KD of 2.9 nM and a Bmax of 6.8 pmol of toxin/mg of protein. Labeled probe can be displaced by unlabeled PbTx-3, PbTx-2, or synthetic PbTx-3 (reduced PbTx-2) but not by a nontoxic, synthetic oxidized derivative of PbTx-2. Competition experiments using natural toxin probes specific for sites 1-4 of the voltage-dependent sodium channel have illustrated that PbTx-3 does not bind to any of the previously described sites associated with the channel. A fifth site is proposed. In addition, because of the varied nomenclature associated with the brevetoxins, a new classification system is proposed.
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Citations
Cited by
Voltage-gated ion channels and gating modifier toxins
Catterall, W. A., Cestèle, S., Yarov-Yarovoy, V., Yu, F. H., Konoki, K., & Scheuer, T. (2007) · Toxicon · doi:10.1016/j.toxicon.2006.09.022 · Cited by 640
The changing face of ciguatera
Lewis, R. J. (2001) · Toxicon · doi:10.1016/s0041-0101(00)00161-6 · Cited by 332
Neurotoxins from Marine Dinoflagellates: A Brief Review
Wang, D.-Z. (2008) · Marine Drugs · doi:10.3390/md6020349 · Cited by 375
Naar, J., Bourdelais, A., Tomas, C., Kubanek, J., Whitney, P. L., Flewelling, L., Steidinger, K., Lancaster, J., & Baden, D. G. (2002) · Environmental Health Perspectives · doi:10.1289/ehp.02110179 · Cited by 177
Self-citationBiotoxin contamination and shellfish safety
Hégaret, H., Wikfors, G. H., & Shumway, S. E. (2009) · Shellfish Safety and Quality · doi:10.1533/9781845695576.1.43 · Cited by 24
Metadata
- Authors
- Poli, M. A., Mende, T. J., & Baden, D. G.
- Venue
- Molecular Pharmacology
- Publisher
- Elsevier BV
- Published
- 1986-08
- Volume
- 30
- Issue
- 2
- Pages
- 129-135
- ISSN
- 0026-895X (ISSN-L)
- OpenAlex
- W2409928090
- Cited by
- 324
- References
- 0
- FWCI
- 2.62
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: Brevetoxins, unique activators of voltage-sensitive sodium channels, bind to specific sites in rat brain synaptosomes. https://app.cochat.ai/papers/10.1016/s0026-895x(25)10324-6
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- Poli, M. A., Mende, T. J., & Baden, D. G. (1986). Brevetoxins, unique activators of voltage-sensitive sodium channels, bind to specific sites in rat brain synaptosomes. Molecular Pharmacology. https://doi.org/10.1016/s0026-895x(25)10324-6
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