The in vitro muscarinic activity and a model for binding to the ml receptor are presented for a series of azaspirodioxolanes.Central activity or blood brain barrier penetration is a prerequisite for any muscarinic agonist which is to have therapeutic potential for Alzheirner's Disease (AD). The potent agonists muscarine and cisdioxolane (CD) are quaternary ammonium compounds which do not penetrate into the CNS. Furthermore the corresponding nor- tertiary amine analogs of these agonists are only weakly active. As part of a program to test muscarinic agonists in AD, we set out to prepate spirocyclic nonquatemary dioxolane analogs and determine if potent CNS active compounds of this substance class were in fact accessible.