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Action of Organophosphate Anticholinesterases on the Three Conformational States of Nicotinic Receptor

  • Mugen Chi
  • Manji Sun
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 363)

Abstract

Organophosphate and other ligands were examined for binding on the membrane-bond nicotinic receptor at three conformational states. Soman (pinacolyl methylphosphonofluoridate), sarin (isopropyl methylphosphonofluoridate, tabun (ethyl N-dimethylphosphoramidocyanidate) and phencyclidine did not show any effect on the binding of [25I]α-cobrotoxin to the nicotinic receptor. However, VX, O-ethyl-S-(2-diisopropylaminoethyl) methylphosphonothiolate, at concentrations higher than 10 umol/L exhibited profound inhibition on the equilibrium binding rates in a concentration-dependent manner. Agonist nicotine and antagonist d-tubocurarine also showed significant inhibitions.

Keywords

Nicotinic Receptor Conformational State Total Binding Electric Organ Binding Rate 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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References

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Copyright information

© Springer Science+Business Media New York 1995

Authors and Affiliations

  • Mugen Chi
    • 1
  • Manji Sun
    • 1
  1. 1.Institute of Pharmacology and ToxicologyBeijingChina

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