SUVN-911 是一种高效、选择性的,有大脑通透性和口服生物活性的神经元烟碱乙酰胆碱 α4β2 受体 (α4β2 receptor) 拮抗剂,Ki值为 1.5 nM。SUVN-911 具有抗抑郁作用。
生物活性 | SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholineα4β2 receptorantagonist, with aKiof 1.5 nM. SUVN-911 has antidepressant activity[1]. |
IC50& Target | Ki: 1.5 nM (α4β2 receptor)[1] |
体外研究 (In Vitro) | SUVN-911 displays high selectivity for α4β2 over α3β4 nAChR[1]. SUVN-911 shows good selectivity against over 70 receptors which includes GPCRs, ion channels, enzymes, peptides, steroids, second messengers, growth factors and prostaglandins[1].
|
体内研究 (In Vivo) | SUVN-911 is devoid of cardiovascular and gastrointestinal side effects[1]. SUVN-911 (1.0-10.0 mg/kg; p.o.; daily; for 3 days) shows significant antidepressant effects[1]. SUVN-911 shows metabolic stability in rats[1]. SUVN-911 (3 mg/kg; p.o.) has shown high oral exposures, longer half-lives and adequate brain penetration in Wistar rats[1].
Animal Model: | Male Wistar rats (180-230 g)[1] | 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)[1] | Dosage: | 3 mg/kg (Pharmacokinetic Analysis) | Administration: | Oral administration | Result: | AUC=3507 ng*h/mL, T1/2=3.34 hours. |
|
Clinical Trial | |
分子量 | |
性状 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 125 mg/mL(478.65 mM;Need ultrasonic) 配制储备液 1 mM | 3.8292 mL | 19.1461 mL | 38.2922 mL | 5 mM | 0.7658 mL | 3.8292 mL | 7.6584 mL | 10 mM | 0.3829 mL | 1.9146 mL | 3.8292 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 |