Skip to main content

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

  • Chapter
Neurochemistry in Clinical Application

Part of the book series: Advances in Experimental Medicine and Biology ((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.

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 39.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 54.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. McNamara, BP et al: (1954) Studies on the mechanism of action of DFP and TEPP. J. Pharmacol. Exp. Ther. 110: 232–334.

    PubMed  CAS  Google Scholar 

  2. Kuba, K and Albuquerque, EX: (1973) Diisopropy fluorophosphate: suppression of ionic conductance of the cholinergic receptor. Science 181: 853–856.

    Article  PubMed  CAS  Google Scholar 

  3. Bakry, NMS et al: (1988) Direct actions of organophosphate anticholinesterases on nicotinic and muscarinic acetylcholine receptor by diisopropylfluophophate. J. Biochem. Toxicol. 3: 235–259.

    Article  PubMed  CAS  Google Scholar 

  4. Eldefrawi, ME et al: (1988) Desensitization of the nicotinic acetylcholine receptor by diisopropylfluophosphate. J. Biochem. Toxicol. 3: 21–32.

    Article  PubMed  CAS  Google Scholar 

  5. Xu, HP et al: (1984) Purification of nicotinic cholinergic receptor protein from the electric organ of Torpediniforms Nadine timilei. Acta Biochem. Biophys. Sinica 16: 50–55.

    CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 1995 Springer Science+Business Media New York

About this chapter

Cite this chapter

Chi, M., Sun, M. (1995). Action of Organophosphate Anticholinesterases on the Three Conformational States of Nicotinic Receptor. In: Tang, L.C., Tang, S.J. (eds) Neurochemistry in Clinical Application. Advances in Experimental Medicine and Biology, vol 363. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-1857-0_9

Download citation

  • DOI: https://doi.org/10.1007/978-1-4615-1857-0_9

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4613-5754-4

  • Online ISBN: 978-1-4615-1857-0

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics