SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity.IC50 & Target: Ki: 1.5 nM (α4β2 receptor)In Vitro: SUVN-911 displays high selectivity for α4β2 over α3β4 nAChR.
SUVN-911 shows good selectivity against over 70 receptors which includes GPCRs, ion channels, enzymes, peptides, steroids, second messengers, growth factors and prostaglandins.
In Vivo: SUVN-911 is devoid of cardiovascular and gastrointestinal side effects.
SUVN-911 (1.0-10.0 mg/kg; p.o.; daily; for 3 days) shows significant antidepressant effects.
SUVN-911 shows metabolic stability in rats.
SUVN-911 (3 mg/kg; p.o.) has shown high oral exposures, longer half-lives and adequate brain penetration in Wistar rats.