Abstract
A series of choline analogues and esters of choline have been evalulated for their ability to antagonize a neuromuscular blockade produced by the hemicholinium (HC-3). The structure of choline appeared to be quite specific for antagonism and any increase in volume about the cationic head or hydroxyl group, increasing or shortening the oxygen to nitrogen interatomic distance or substitution on the carbon chain resulted in loss of activity. Choline esters were effective antagonists, but this property was blocked by pretreatment with TEPP, indicating that choline was the active agent. The antagonistic ability of acetvlcholine was diminished by pretreatment with TEPP but not with neostigmine.
Footnotes
- Received March 28, 1959.
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