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].
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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. |
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| 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。 |
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