Synthesis and Pharmacological Characterization of exo-2-(2'-Chloro-5-pyridinyl)-7-(endo and exo)-aminobicyclo[2.2.1]heptanes as Novel Epibatidine Analogues

摘要

Procedures were developed for the synthesis of exo-(2'-chloro-5-pyridinyl)-7-(endo and exo)-amino[2.2.1]heptanes(3a and 3b).The compounds were evaluated for binding to the alpha4beta2 and alpha7 nicotinic acetylcholine receptors(nAChRs),for pharmacological activity in the mouse tail-flick and hot-plate assays,and for hypothermia and locomotor activity.Compounds 3a and 3b possessed alpha 4 beta 2 nAChR binding properties similar to those of(-)-nicotine and were nAChR agonists in all four mouse assays.