(S)-WAY-100135 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT (IC = 15.5 nM in a radioligand binding assay using rat hippocampus). It is selective for 5-HT over 5-HT, 5-HT, and 5-H receptors, as well as dopamine D and D, and α-, α-, and β-adrenergic receptors (ICs = >1 µM for all). (S)-WAY-100135 (10 mg/kg) increases the number of entries into and percentage of time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity.
(S)-WAY 100135 dihydrochloride is a highly selective and potent antagonist of 5-HT 1A (IC50=33.9 nM). (S)-WAY 100135 dihydrochloride has anxiolytic activity in animal models.