Sparteine作为抗惊厥药：证据和可能的作用机理。,Seizure: European Journal of Epilepsy

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Sparteine作为抗惊厥药：证据和可能的作用机理。
Seizure: European Journal of Epilepsy ( IF 2.7 ) Pub Date : 2016-06-06 , DOI: 10.1016/j.seizure.2016.05.010
Fridha Villalpando-Vargas ₁ , Laura Medina-Ceja ₁

Affiliation

Sparteine是一种从羽扇豆提取的喹oli嗪生物碱，在人类和动物模型中均具有众多药理特性。在中枢神经系统中，sparteine会降低运动能力，具有轻微的镇痛作用，也不会影响短期记忆或空间学习，并且不会引起行为或脑电图（EEG）活动的改变。但是，在实验动物中并未充分表征斯巴丁胺的抗惊厥作用，并且在人类中尚无数据。因此，本综述着重于在急性癫痫发作和癫痫持续状态（SE）模型中支持斯巴丁胺的抗惊厥作用的实验证据，以及其可能的作用机理。支持硫酸-（-）-天冬氨酸的抗惊厥作用的证据包括抑制最大电刺激诱发的癫痫发作，惊厥行为发作的延迟和戊四氮唑（PTZ）治疗小鼠的存活时间延长。此外，斯巴汀会延缓惊厥行为的发作，并降低接受PTZ和毛果芸香碱治疗的大鼠的严重程度和死亡率。Sparteine可降低振幅和频率或阻止PTZ，毛果芸香碱和海藻酸诱导的癫痫样活动。Sparteine可能通过激活mAChR的M2和M4亚型来降低过度兴奋性，这是一种可能的作用机制，其全身作用可能有利于其抗惊厥和SE的抗惊厥作用。戊四唑（PTZ）处理的小鼠惊厥行为的延迟和存活时间的延长。此外，斯巴汀会延缓惊厥行为的发作，并降低接受PTZ和毛果芸香碱治疗的大鼠的严重程度和死亡率。Sparteine可降低振幅和频率或阻止PTZ，毛果芸香碱和海藻酸诱导的癫痫样活动。Sparteine可通过激活mAChR的M2和M4亚型来降低过度兴奋性，这是一种可能的作用机理，其全身作用可能有利于其抗惊厥和SE的抗惊厥作用。戊四唑（PTZ）处理的小鼠惊厥行为的延迟和存活时间的延长。此外，斯巴汀会延缓惊厥行为的发作，并降低接受PTZ和毛果芸香碱治疗的大鼠的严重程度和死亡率。Sparteine可降低振幅和频率或阻止PTZ，毛果芸香碱和海藻酸诱导的癫痫样活动。Sparteine可能通过激活mAChR的M2和M4亚型来降低过度兴奋性，这是一种可能的作用机制，其全身作用可能有利于其抗惊厥和SE的抗惊厥作用。司巴汀会延缓惊厥行为的发作，并降低接受PTZ和毛果芸香碱治疗的大鼠的严重程度和死亡率。Sparteine可降低振幅和频率或阻止PTZ，毛果芸香碱和海藻酸诱导的癫痫样活动。Sparteine可能通过激活mAChR的M2和M4亚型来降低过度兴奋性，这是一种可能的作用机制，其全身作用可能有利于其抗惊厥和SE的抗惊厥作用。司巴汀会延缓惊厥行为的发作，并降低接受PTZ和毛果芸香碱治疗的大鼠的严重程度和死亡率。Sparteine可降低振幅和频率或阻止PTZ，毛果芸香碱和海藻酸诱导的癫痫样活动。Sparteine可能通过激活mAChR的M2和M4亚型来降低过度兴奋性，这是一种可能的作用机制，其全身作用可能有利于其抗惊厥和SE的抗惊厥作用。

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Sparteine as an anticonvulsant drug: Evidence and possible mechanism of action.

Sparteine is a quinolizidine alkaloid extracted from Lupinus that has numerous pharmacological properties both in humans and animal models. In the central nervous system, sparteine reduces locomotor activity, has light analgesic effects, also has no effects on short-term memory or spatial learning and does not induce changes in behavior or electroencephalographic (EEG) activity. However, the anticonvulsant profile of sparteine is not fully characterized in experimental animals and there are no data in humans. Therefore, the present review focuses on the experimental evidence supporting the anticonvulsant action of sparteine in models of acute seizures and status epilepticus (SE), as well as its possible mechanisms of action. The evidence that supports the anticonvulsant effect of (-)-Sparteine sulfate includes the inhibition of seizures induced by maximal electro-stimulation, a delay in the onset of convulsive behavior and the prolongation of survival time in mice treated with pentylenetetrazole (PTZ). Additionally, sparteine delays the onset of convulsive behavior and decreases the severity and mortality of rats treated with PTZ and pilocarpine. Sparteine decreases amplitude and frequency or blocks the epileptiform activity induced by PTZ, pilocarpine and kainic acid. Sparteine may decrease hyperexcitability through the activation of the M2 and M4 subtypes of mAChRs, which is a probable mechanism of action that together with its systemic effects may favor its anticonvulsant effects against seizures and SE.

更新日期：2019-11-01

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