Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptors

Indoles 11 and 12 (R1 and/or R2 = NHCH3 or H; R and R3 = NH2 or H) were examined to determine the influence of amine substituents on 5-HT6 receptor affinity. Although all compounds displayed low nanomolar affinity, only a single aryl amine moiety is required for binding. It appears that multiple modes of binding are possible upon interaction of these types of compounds with 5-HT6 receptors.