Picrotoxin-mediated antagonism of α3β4 and α7 acetylcholine receptors

Brian E. Erkkila, David S. Weiss, Virginia E. Wotring

Research output: Contribution to journalArticle

17 Scopus citations

Abstract

Picrotoxin (PTX) is a convulsant that antagonizes many inhibitory ligand-gated receptors. The mechanism of PTX block is believed to involve residues which line the pore in the second transmembrane domain (M2). The α3β4 and α7 nicotinic acetylcholine receptors (nAChRs) have high homology to inhibitory LGICs in this M2 region and therefore could also be susceptible to block by PTX. Here, we report that PTX is an effective inhibitor at these nicotinic receptors (rat), with IC50 values of 96.1 ± 5.5 and 194.9 ± 19.2 μM for the α3β4 and α7, respectively. These results provide insights into the structure-function relation of PTX-mediated antagonism in this family of ligand-activated receptors. Furthermore they should also be considered when employing PTX to selectively eliminate GABA- or glycine-mediated events.

Original languageEnglish (US)
Pages (from-to)1969-1973
Number of pages5
JournalNeuroReport
Volume15
Issue number12
DOIs
StatePublished - Aug 26 2004
Externally publishedYes

Keywords

  • Acetylcholine
  • GABA receptor
  • Ligand-gated ion channel
  • Nicotinic receptor
  • Picrotoxin

ASJC Scopus subject areas

  • Neuroscience(all)

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