PHARMACOLOGIC STUDIES ON SOME COMPOUNDS STRUCTURALLY RELATED TO THE HEMICHOLINIUM HC-3

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

A series of HC-3 analogs featuring alterations in the side chains and nucleus has been studied. Their ability to inhibit acetylcholinesterase, salivary flow in the dog and muscular contraction in the rabbit following electrical stimulation of the chorda tympani and sciatic nerves has been evaluated. The data obtained from the neuromuscular preparations were statistically analyzed and the relative potency of the analogs in relation to the standard (HC-3) was determined. The structure activity relationships of the analogs with respect to their relative potency as neuromuscular blocking agents have been discussed. No compounds were encountered which were as active as HC-3. In addition, some of the analogs were effective inhibitors of acetylcholinesterase.