Product Introduction
Bioactivity


英文名: 6-Benzoylheteratisine

描述: 6-Benzoylheteratisine (Heteratisan-14-one, 6-(benzoyloxy)-20-ethyl-8-hydroxy-1-methoxy-4-meth) 是乌头碱的拮抗剂，乌头碱是天然 Na+通道激活剂。

体外活性: 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。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 25 mg/mL (50.44 mM)


关键字: Inhibitor | 6Benzoylheteratisine | Sodium Channel | inhibit | Na+ channels | 6-Benzoylheteratisine | Na channels | 6 Benzoylheteratisine

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相关库: Anti-Cancer Compound Library | Selected Plant-Sourced Compound Library | Natural Product Library for HTS | Sodium Channel Blocker Library | RO5 Drug-like Natural Product Library | NO PAINS Compound Library | Natural Product Library