(Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonists

CNS-active aminotetralins containing phenolic moieties were transformed in a simple two-step procedure to the corresponding benzofurans. The compounds were tested in in vitro binding studies at serotonin 5-HT1A and 5-HT2 and dopamine D2, D3 and D4 receptors. These studies revealed that the furan homologs showed overall lower affinities than the phenol counterparts. This was also reflected in vivo in biochemical studies. The benzofuran compounds retained most of the agonist/antagonist activities but with lower potency.