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.
体外研究
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.
体内研究
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.
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, T1/2=3.34 hours.
分子式
C11H14Cl2N2O
分子量
261.15
CAS号
2414674-71-6
运输条件
Room temperature in continental US; may vary elsewhere.