Masupirdine (free base)

Masupirdine free base (SUVN-502 free base) is a potent, selective, orally active, and brain-penetrating 5-HT₆ receptor antagonist (K_i of 2.04 nM for human 5-HT₆ receptor). Masupirdine free base has pro-cognitive effects on all stages of cognition (acquisition, consolidation, and retention), and can reverse Scopolamine (HY-N0296), MK-801 (HY-15084B)-induced and aging-related memory deficits. Masupirdine free base can be used in the research of Alzheimer's disease^[1][2]. IC50 & Target:Ki: 2.04 nM (human 5-HT6 receptor)^[1] In Vitro:Masupirdine (10 μM) free base shows no agonist or partial agonist effects on luciferase activity but blocks serotonin-induced luciferase activity in the 5-HT₆ receptor functional assay using CHO-K1 cells stably expressing human 5-HT₆ receptor and CRE-Luc reporter gene^[2].
In Vivo:Masupirdine (1-10 mg/kg; p.o) free base exerts procognitive effects on acquisition, consolidation, and retention phases of memory in adult male Wistar rats, and reverses memory deficits induced by Scopolamine (HY-N0296), Scopolamine/MK-801 (HY-15084B), or senescence^[2].