A Screening Program for Selective Inhibitors of the Phosphorylation of Acetylcholinesterase.
Abstract
Thirty-one structurally diverse compounds were examined for their ability to inhibit cholinesterases from eel and rat brain. Inhibition was measured in terms of rate of substrate hydrolysis (acetylcholine and acetylthiocholine) and in rate of phosphorylation by Tetram (O,O-diethyl S-2-diethylaminoethyl phosphorothioate). It is suggested that compounds which preferentially inhibit phosphorylation may have possible value in prophylaxis of poisoning by organophosphorus anticholinesterases. The kinetics of the interaction of enzyme with substrates and inhibitors is examined. Three compounds are suggested for examination in test animals. (Author)
Document Details
- Document Type
- Technical Report
- Publication Date
- Nov 01, 1973
- Accession Number
- AD0771149
Entities
People
- George M. Steinberg
- Joseph W. Amshey Jr.
- Robert B. Miller