Actions of synthetic piperidine derivatives on an insect acetylcholine receptor/ion channel complex

J. A. David, P. J. Crowley, S. G. Hall, M. Battersby, D. B. Sattelle*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

9 Citations (Scopus)

Abstract

The actions of synthetic piperidine derivatives on the response to ionophoretically-applied acetylcholine (ACh) have been tested on the cell body membrane of the fast coxal depressor motoneurone (Ff) of the cockroach Periplaneta americana. The cis form and the cis (80%):trans (20%) mixture of 2-methyl-6-undecyl piperidine were the most effective (the half-maximal blocking action of the mixed isomers was estimated to be 6.3 × 10-5 M). Less potent was the cis (50%):trans (50%) mixture of 2-methyl-6-tridecyl piperidine. However, pure cis 2-methyl-6-tridecyl piperidine was even less effective than the mixed isomers, indicating that, in the case of the tridecyl derivative, the trans form was largely responsible for the block of the ACh response. Cis 2-Methyl-6-undecyl piperidine failed to inhibit the binding of N-[propionyl-3H] propionylated α-bungarotoxin to metathoracic ganglion homogenates at concentrations up to 1.0 × 10-4 M. Also, block of ACh-induced current by 2-methyl-6-undecyl piperidine (cis 80%:trans 20%) was largely independent of membrane potential in the range -120 mV to -60 mV, indicating an interaction with the closed ACh receptor/ion channel complex at a site which, in the case of the cis isomer, is separate from the binding site for α-bungarotoxin.

Original languageEnglish
Pages (from-to)191-196
Number of pages6
JournalJournal of Insect Physiology
Volume30
Issue number3
DOIs
Publication statusPublished - 1984

Keywords

  • acetylcholine receptor
  • CNS
  • electrophysiology
  • fast coxal depressor motoneurone
  • Periplaneta americana
  • radiolabelled ligand binding
  • Synthetic piperidines

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