SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a K i of 1.5 nM. SUVN-911 has antidepressant activity
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Wistar rats (180-230 g) Dosage: 1 mg/kg, 3 mg/kg, 10.0 mg/kg Administration: Oral administration, daily, for 3 days Result: Showed antidepressant like activity with no signs of tachyphylaxis. Animal Model: Male Wistar rats (225 ± 25 g) Dosage: 3 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration Result: AUC=3507 ng*h/mL, T 1/2 =3.34 hours.
Form:Solid
IC50& Target:Ki: 1.5 nM (α4β2 receptor)
