DSP-1053

DSP-1053 is a novel potent serotonin reuptake (SERT) inhibitor with 5-HT1A partial agonistic activity that binds to human serotonin transporter and 5-HT1A receptor with Ki of 1.02 and 5.05 nM, respectively; inhibits serotonin transporter with IC50 of 2.74 nM and shows an intrinsic activity for 5-HT1A receptors of 70.0%; dose-dependently increases extracellular 5-HT levels in rat microdialysis at 3-10 mg/kg, demonstrates antidepressant-like effect in vivo. Depression Phase 1 Discontinued

References 1. Yoshinaga H, et al. Bioorg Med Chem. 2018 May 1;26(8):1614-1627. 2. Kato T, et al. Pharmacol Res Perspect. 2015 Jun;3(3):e00142. View Related Products by Target 5-HT Receptor Depression