1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands

4-Arylsulfone derivatives of 1-(1-naphthyl)piperazine represent a novel class of human 5-HT6 serotonin receptor ligands. In particular, compounds such as 1f (1; R = H; Ki = 3.8 nM) and 1g (1; R = NH2; Ki = 0.9 nM) displayed high affinity for this receptor population, and 1f was shown to behave as a 5-HT6 antagonist.