Kinetics of inhibition of acetylcholinesterase by spin labeled acetylcholine analogs.


Journal Article

A series of spin labeled acetycholine analogs, in which the number of methylene groups between the quaternary nitrogen and the alcohol oxygen ranged between 1-5, have been examined as inhibitors of electric eel acetylcholinesterase. Evidence is presented suggesting that inhibition of acetylocholinesterase by the spin labeled ACH analogs is due to the high affinity of these compounds for the enzyme, inhibition is competitive and reversible. It has been shown that complex formation is of major importance in the reaction between spin labeled ACH analogs and acetylcholinesterase. The acetylation step has been shown to occur by demonstrating that the leaving group is released as the reaction proceeds. Complex formation has been demonstrated by means of kinetic criteria. Kinetic parameter have been measured for the five compounds, and correlations with alkaline hydrolysis are disussed.

Full Text

Duke Authors

Cited Authors

  • Abou-Donia, MB; Rosen, GM

Published Date

  • December 1, 1976

Published In

Volume / Issue

  • 6 / 1

Start / End Page

  • 15 - 21

PubMed ID

  • 1035114

Pubmed Central ID

  • 1035114

International Standard Serial Number (ISSN)

  • 0301-4622

Digital Object Identifier (DOI)

  • 10.1016/0301-4622(76)80057-9


  • eng

Conference Location

  • Netherlands