Wf-516 is a 5-HT reuptake inhibitor (Kis: 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively), and with potent antidepressant activity.

5-HT2A receptor (human):40 nM (ki), 5-HT1A receptor (human):ki:5 nM

Wf-516 shows high affinity for 5-HT1A receptors in the hippocampus and raphe nucleus of rats(Ki of 8.1 nM and 7.9 nM, respectively)[2].

Wf-516 (0.5 mg/kg, i.v.) does not induce any change in the firing activity of 5-HT neurons, but significantly blocks the inhibitory effect of 8-OHDPAT (a 5-HT autoreceptor agonist) by 70%. A full dose-response relationship between the suppression of DRN firing activity and different doses of LSD shows a significant fourfold shift to the right in the Wf-516 pretreated rats (ED50?=?32.4?±?1.0 μg/kg) as compared to controls with ED50?of?7.5?±?1.2 μg/kg. After intravenous administration of successive doses of 1.25 mg/kg of Wf-516 (up to 10 mg/kg), the effect of microiontophoretically applied 5-HT is prolonged and reaches statistical significance at 7.5 mg/kg. At this dose, the RT50 value is increased by 53% and, by 75% at the highest dose of 10 mg/kg of Wf-516 used[1].Compared with baseline, oral administration of 30 mg/kg Wf-516 to these 5,7-DHT-treated rats induced a significant decrease in hippocampal BPND, but no further decrease in BPND was observed in the grooved nuclei. The oral ED50 values of Wf-516 in the hippocampus and grooved nuclei were 5.3 mg/kg and 4.2 mg/kg, respectively [2].