Differential effects of five 'classical' scorpion β-toxins on rNav1.2a and DmNav1 provide clues on species-selectivity

Frank Bosmans, Marie France Martin-Eauclaire, Jan Tytgat

Research output: Contribution to journalArticlepeer-review

25 Scopus citations

Abstract

In general, scorpion β-toxins have been well examined. However, few in-depth studies have been devoted to species selectivity and affinity comparisons on the different voltage-activated Na+ channels since they have become available as cloned channels that can be studied in heterologous expression systems. As a result, their classification is largely historical and dates from early in vivo experiments on mice and cockroach and fly larvae. In this study, we aimed to provide an updated overview of selectivity and affinity of scorpion β-toxins towards voltage-activated Na+ channels of vertebrates or invertebrates. As pharmacological tools, we used the classic β-toxins AaHIT, Css II, Css IV, Css VI and Ts VII and tested them on the neuronal vertebrate voltage-activated Na+ channel, rNav1.2a. For comparison, its invertebrate counterpart, DmNav1, was also tested. Both these channels were expressed in Xenopus laevis oocytes and the currents measured with the two-electrode voltage-clamp technique. We supplemented this data with several binding displacement studies on rat brain synaptosomes. The results lead us to propose a general classification and a novel nomenclature of scorpion β-toxins based on pharmacological activity.

Original languageEnglish (US)
Pages (from-to)45-51
Number of pages7
JournalToxicology and Applied Pharmacology
Volume218
Issue number1
DOIs
StatePublished - Jan 1 2007
Externally publishedYes

Keywords

  • Androctonus australis Hector
  • Centruroides suffusus suffusus
  • Scorpion β-toxins
  • Species-selectivity
  • Voltage-activated Na channels

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology

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