SUVN-911
| CAS号 | 2414674-71-6 | 货号 | BCP32917 |
| 中文名 | SUVN-911 | ||
| 英文名 | SUVN-911 | ||
| 中文别名 | |||
| 英文别名 | SUVN911;SUVN 911; | ||
| 分子式 | C11H14Cl2N2O | 分子量 | 261.14 |
| 生物活性 | SUVN-911 is a Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression.SUVN-911 is a potent α4β2 receptor ligand with a Ki value of 1.5 nM. It showed >10 μM binding affinity toward the ganglionic α3β4 receptor apart from showing selectivity over 70 other targets. It is orally bioavailable and showed good brain penetration in rats. Marked antidepressant activity and dose-dependent receptor occupancy in rats support its potential therapeutic utility in the treatment of depression. It does not affect the locomotor activity at doses several folds higher than its efficacy dose. It is devoid of cardiovascular and gastrointestinal side effects. Successful long-term safety studies in animals and phase-1 evaluation in healthy humans for safety, tolerability, and pharmacokinetics paved the way for its further development. | ||
| 信号通路 | Ion Channel/Membrane Transporter Neuro Signaling Pathway | ||
| 靶 点 | nAChR | ||
结构式
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