Serotonergic and dopaminergic activities of rigidified (R)-aporphine derivatives

Novel rigidified (R)-aporphine derivatives were synthesized from (R)-1,11-carbonylaporphine by ring expansion reactions. The structures of the novel analogues were assigned by NMR spectroscopy and X-ray crystallography. The compounds showed moderate affinities and selectivities at serotonin 5-HT1A and 5-HT7 and dopamine D2A receptors.