SUVN-911 是高选择性的,大脑通透性的和口服有效的神经元烟碱乙酰胆碱 α4β2 受体拮抗剂,Ki为 1.5 nM。SUVN-911显示出抗抑郁作用。
产品描述
suvn-911 is a potent and selective antagonist of neuronal nicotinic acetylcholine α4β2 receptor (Ki = 1.5 nM) with antidepressant activity.
体外活性
suvn-911 shows good selectivity against over 70 receptors which includes GPCRs, ion channels, enzymes, peptides, steroids, second messengers, growth factors, and prostaglandins. suvn-911 displays high selectivity for α4β2 over α3β4 nAChR[2].
体内活性
In male Wistar rats, suvn-911 (1.0-10.0 mg/kg; p.o.) showed significant antidepressant-like activity with no signs of tachyphylaxis. suvn-911 (3 mg/kg; p.o.) showed high oral exposures, longer half-lives(T1/2 = 3.34 hr), and adequate brain penetration in Wistar rats. suvn-911 showed metabolic stability and no cardiovascular and gastrointestinal side effects[1].
Cas No.
2414674-71-6
别名
suvn-911
储存和溶解度
DMSO:125 mg/mL (478.65 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years