Agonist pharmacology of the neuronal alpha 7 nicotinic receptor expressed in Xenopus oocytes

FEBS Lett. 1993 Aug 2;327(3):284-8. doi: 10.1016/0014-5793(93)81005-k.

Abstract

The potencies and efficacies of seven agonists at chick alpha 7 nicotinic receptors expressed in Xenopus oocytes were determined by whole cell recording. (+)-Anatoxin-a was the most potent agonist (EC50 = 0.58 microM) and acetylcholine was the least potent (EC50 = 320 microM). The rank order of agonist potencies was: (+)-anatoxin-a >> cytisine > (-)-nicotine > (+)-nicotine > DMPP > 1-acetyl-4-methylpiperazine methiodide > acetylcholine. DMPP evoked only very small currents: comparison of maximally effective agonist concentrations showed that DMPP was only one-fifth as efficacious as other agonists. Previously published IC50 values for rat brain [125I]alpha-bungarotoxin sites show a similar agonist profile, and the identity of homo-oligomeric alpha 7 receptors with native alpha-bungarotoxin-sensitive neuronal nicotinic receptors is discussed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholine / pharmacology
  • Alkaloids / pharmacology
  • Animals
  • Azocines
  • Bacterial Toxins / pharmacology
  • Cyanobacteria Toxins
  • DNA
  • Dimethylphenylpiperazinium Iodide / pharmacology
  • Marine Toxins / pharmacology
  • Membrane Potentials
  • Microcystins
  • Neurons / metabolism*
  • Neurons / physiology
  • Nicotine / pharmacology
  • Oocytes
  • Piperazines / pharmacology
  • Quaternary Ammonium Compounds*
  • Quinolizines
  • Receptors, Nicotinic / drug effects*
  • Receptors, Nicotinic / genetics
  • Tropanes
  • Xenopus

Substances

  • Alkaloids
  • Azocines
  • Bacterial Toxins
  • Cyanobacteria Toxins
  • Marine Toxins
  • Microcystins
  • Piperazines
  • Quaternary Ammonium Compounds
  • Quinolizines
  • Receptors, Nicotinic
  • Tropanes
  • cytisine
  • Dimethylphenylpiperazinium Iodide
  • 1,1-dimethyl-4-acetylpiperazinium
  • Nicotine
  • anatoxin a
  • DNA
  • Acetylcholine