Epibatidine structure–activity relationships

Epibatidine is a potent but nonselective nAChR agonist. Its biological effects appear to be mediated largely by α4β2 nAChRs. Surprisingly, only a limited number of epibatidine analogues have been synthesized and evaluated in in vitro assays. Even fewer analogues have received in vivo pharmacological evaluation. In this paper, SAR studies directed toward epibatidine analogues will be reviewed.