WAY-181187 is a high affinity and selective 5-HT6 agonist. It displays 60-fold selectivity over other 5-HT and monoamine receptors. WAY-181187 stimulates cAMP, ERK1/2 and Fyn kinase signaling pathway through serotonin receptor activation. WAY-181187 produced both antidepressant-like and anxiolytic-like effects in the animal model. It had been in phase I clinical trial for the treatment of anxiety disorders but this research has been discontinued.

WAY 208466 dihydrochloride is a high affinity, selective SR-6 (5-HT6) receptor agonist. WAY-208466 produced both antidepressant-like and anxiolytic-like effects. Direct infusion of WAY-208466 into the dorsal raphe nucleus, locus coeruleus, basal forebrain (horizontal limb of the diagonal band of Broca) or laterodorsal tegmental nucleus specifically decreased REM sleep without significantly altering wakefulness or slow wave sleep.