Picrotoxinin binding sites at the GABA synapse: A target for drug action

M. K. Ticku, R. W. Olsen

Research output: Contribution to journalArticlepeer-review

13 Scopus citations


α-Dihydropicrotoxinin (DHP), a GABA synaptic antagonist, binds to rat brain and crayfish membranes with an apparent KD of 1-2 μ.M. Based on several lines of evidence, it appears that DHP binds to GABA-receptor-ionophore complex at a site distinct from the GABA receptor sites. A variety of centrally acting depressant and convulsant drugs which affect GABAergic transmission inhibit DHP and not GABA binding. The data suggest that DHP-sensitive site at the GABA receptor ionophores may be involved not only in drug action but in possible regulation of the chloride ionophores.

Original languageEnglish (US)
Pages (from-to)213-216
Number of pages4
JournalBrain Research Bulletin
Issue numberSUPPL. 2
StatePublished - 1980


  • Convulsants
  • Depressants
  • Dihydropicrotoxinin
  • GABA
  • Ionophore
  • Receptor

ASJC Scopus subject areas

  • Neuroscience(all)


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