Synthesis and Pharmacological Properties of N-Decyltropine (IEM-1556) as Compared to Selective Nicotinic Receptor Antagonist Tert-Butyldecylammonium (IEM-1678)

Resumo

The property profile of N-decyltropine (IEM-1556) has significant advantages over that of its prototype, the selective nicotinic receptor antagonist tert-butyldecylammonium (IEM-1678), because its anticonvulsant, antiparkinsonian, antidepressant, and analgesic activities are significantly greater and its therapeutic index is 2.8 times higher than that of IEM-1678. The higher pharmacological activity and lower toxicity of IEM-1556 are explained by the fact that IEM-1556 not only blocks nicotinic receptors but also stimulates subdiaphragmatic vagal afferents.