Биологическая активность
SUVN-911 (compound 9h) is a Novel, мощный, селективный, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 рецептор антагонист for the Treatment of Depression.Compound 9h is a мощный α4β2 рецептор лиганд with a Ki value of 1.5 nM. It showed >10 μM связывание affinity toward the ganglionic α3β4 рецептор 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 рецептор 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.
Оригинал на английском
SUVN-911 (compound 9h) is a Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression.Compound 9h 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.
Химические свойства
- CAS №
- 2414674-71-6
- Брутто-формула
- C₁₁H₁₄Cl₂N₂O
- Мол. масса
- 261.15 г/моль
- SMILES
- [C@H]12N[C@H](COC3C=NC(Cl)=CC=3)C[C@H]1C2.[H]Cl
- Синонимы
- 2414674-70-5(free base),SUVN-911,SUVN911,SUVN 911
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.