Биологическая активность
MDL-72274 HCl is селективный and мощный inhibitors of SSAO for treatment of Parkinson diseases. MDL-72974 is a мощный (IC50 = 10(-9) M) ингибитор of both MAO-B and SSAO, with 190-fold lower affinity for MAO-A. In clinical studies, oral doses as low as 100 micrograms produced substantial inhibition of platelet MAO-B. One or 4 mg MDL-72274 HCl given daily for 28 days to 40 Parkinson's patients treated with L-dopa produced statistically significant reductions in the Unified Parkinson's Disease Rating Scale. MAO-B inhibitors, such as MDL 72974A and L-deprenyl, offer the potential of being neuroprotective in Parkinson's Disease and other neurogenerative disorders.
Оригинал на английском
MDL-72274 HCl is selective and potent inhibitors of SSAO for treatment of Parkinson diseases. MDL-72974 is a potent (IC50 = 10(-9) M) inhibitor of both MAO-B and SSAO, with 190-fold lower affinity for MAO-A. In clinical studies, oral doses as low as 100 micrograms produced substantial inhibition of platelet MAO-B. One or 4 mg MDL-72274 HCl given daily for 28 days to 40 Parkinson's patients treated with L-dopa produced statistically significant reductions in the Unified Parkinson's Disease Rating Scale. MAO-B inhibitors, such as MDL 72974A and L-deprenyl, offer the potential of being neuroprotective in Parkinson's Disease and other neurogenerative disorders.
Химические свойства
- CAS №
- 85278-24-6
- Брутто-формула
- C₉H₁₁Cl₂N
- Мол. масса
- 204.09 г/моль
- SMILES
- NC/C(C1=CC=CC=C1)=C/Cl.[H]Cl
- Синонимы
- MDL72274; MDL-72274; MDL 72274; MDL72274A; MDL-72274A и ещё 2
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.