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

Article abstract of DOI:10.1016/S0960-894X(97)10068-3

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-HT(1A) 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 that the furan homologs showed overall lower affinities than the phenol counterparts. This was reflected in vivo in biochemical studies. The benzofuran compounds retained most of the agonist/antagonist activities but with lower potency.