Structure-Activity Relationships of Agents Modifying Cholinergic Transmission

Abstract

Structure activity relationship studies of hemicholinium (HC-3) analogs are directed toward better understanding both the spatial aspect of the receptor and interatomic distances between the 2 cationic heads. Several series of compounds including 4,4'biphenyl and trans/trans-cyclohexyl derivatives are being investigated and both series are potent inhibitors of acetylcholine synthesis. One compound, N-methyl 4-methyl piperidine derivative in the biphenyl series, is a very active inhibitor of ACh synthesis. The tertiary amine analog is an active inhibitor of synthesis of acetylcholine. It is much less active than the quaternary derivative. Recently we discovered that 4-hydroxy-piperidine analogs of hemicholinium have the same therapeutic index for protection of mice against paraoxan-induced toxicity as pyridostigmine. Keywords: Pharmacological antagonists.

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Document Details

Document Type
Technical Report
Publication Date
Apr 01, 1988
Accession Number
ADA197120

Entities

People

  • J. G. Cannon
  • J. P. Long
  • R. K. Bhatnagar

Organizations

  • University of Iowa

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DTIC Thesaurus Topics

  • 1-Ring Heterocyclic Compounds
  • Alcohols
  • Cells
  • Chemical Synthesis
  • Chemistry
  • Confidence Limits
  • Data Analysis
  • Enzyme Inhibitors
  • Information Science
  • Inhibition
  • Inhibitors
  • Isomers
  • Molecules
  • Neuromuscular Transmission
  • Neurons
  • Organic Chemistry
  • Rodents

Fields of Study

  • Chemistry

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  • Neurotoxicology
  • Organic Chemistry
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