| Description | 6-Benzoylheteratisine (Heteratisan-14-one, 6-(benzoyloxy)-20-ethyl-8-hydroxy-1-methoxy-4-meth) is a Aconitum alkaloid. It can inhibits voltage-gated Na+ channels in rat brain synaptosomes |
| In vitro | 6-Benzoylheteratisine对乌头碱诱导的[Na+]i、[Ca2+]i增加及谷氨酸释放具有浓度依赖性抑制效应。IC50值分别为4.1微摩尔(Na+)、4.8微摩尔(Ca2+)和4.8微摩尔(谷氨酸释放)。使用100微摩尔6-Benzoylheteratisine在5微摩尔藜芦碱刺激后也能减少诱导的[Na+]i和[Ca2+]i，其半衰期分别为72.1秒和44.7秒。此外，100微摩尔6-Benzoylheteratisine降低了由歐巴亭诱导的Na+流入，其效果与Na+通道抑制剂河豚毒素相当，这表明6-Benzoylheteratisine通过抑制非激活状态的Na+通道。同样，100微摩尔6-Benzoylheteratisine对30毫摩尔氯化钾诱导的谷氨酸释放和[Ca2+]i增加无影响，表明电压门控性Ca2+通道未受6-Benzoylheteratisine影响。数据表明，6-Benzoylheteratisine对电压门控Na+通道具有抑制效应，而Na+和Ca2+的稳态机制及谷氨酸释放途径似乎不受该药物影响。 |
| Synonyms | Heteratisan-14-one, 6-(benzoyloxy)-20-ethyl-8-hydroxy-1-methoxy-4-meth, 苯甲酰新异乌头碱 |
| molecular weight | 495.61 |
| Molecular formula | C29H37NO6 |
| CAS | 99759-48-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 25 mg/mL (50.44 mM) |
| References | 2. Gutser U T , Gleitz J . The alkaloid 6-benzoylheteratisine inhibits voltage-gated Na+ channels in rat brain synaptosomes.[J]. Neuropharmacology, 1998, 37(9):1139-1146. |