INVESTIGATIONS ON A SERIES OF HETEROCYCLIC HEMICHOLINIUM-3 ANALOGS

¹ Department of Pharmacology, College of Medicine, The University of Iowa, Iowa City, Iowa

Eight substituted pyridinium and N-methylpiperidinium analogs of hemicholinium-3 were evaluated for their ability to block neuromuscular transmission in the rabbit and to inhibit human erythrocyte acetylcholinesterase. The 3-methylpyridinium and 4-methylpiperidinium derivatives were found to be equipotent to hemicholinium-3 as neuromuscular blockers. The low activity of the 3-methylpiperidinium analog is tentatively explained on the basis of enantiomeric dilution coupled with a possible low yield of the active conformer on quaternization.