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评估醋酸艾司利卡西平在减少癫痫GASH/Sal模型中听源性反射性癫痫发作方面的有效性。

Assessing the Effectiveness of Eslicarbazepine Acetate in Reducing Audiogenic Reflex Seizures in the GASH/Sal Model of Epilepsy.

作者信息

Gonçalves-Sánchez Jaime, Ramírez-Santos Thomas, López Dolores E, Gonçalves-Estella Jesús M, Sancho Consuelo

机构信息

Department of Cell Biology and Pathology, School of Medicine, University of Salamanca, 37007 Salamanca, Spain.

Institute for Biomedical Research of Salamanca (IBSAL), 37007 Salamanca, Spain.

出版信息

Biomedicines. 2024 May 18;12(5):1121. doi: 10.3390/biomedicines12051121.

DOI:10.3390/biomedicines12051121
PMID:38791083
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11117828/
Abstract

Eslicarbazepine acetate (ESL) is a third-generation antiepileptic drug indicated as monotherapy for adults with newly diagnosed epilepsy and as adjunctive therapy for the treatment of partial seizures. Our aim was to assess the effectiveness and safety of both acute and repeated ESL administration against reflex audiogenic seizures, as shown by the Genetic Audiogenic Seizures Hamster from Salamanca (GASH/Sal). Animals were subject to the intraperitoneal administration of ESL, applying doses of 100, 150 and 200 mg/kg for the acute study, whereas a daily dose of 100 mg/kg was selected for the subchronic study, which lasted 14 days. In both studies, the anticonvulsant effect of the therapy was evaluated using neuroethological methods. To assess the safety of the treatment, behavioral tests were performed, hematological and biochemical liver profiles were obtained, and body weight was monitored. In addition, the ESL levels in blood were measured after the acute administration of a 200 mg/kg dose. Treatment with ESL caused a reduction in seizure severity. No statistically significant differences were detected between the selected doses or between the acute or repeated administration of the drug. To summarize, the intraperitoneal administration of ESL is safe and shows an anticonvulsant effect in the GASH/Sal.

摘要

醋酸艾司利卡西平(ESL)是一种第三代抗癫痫药物,适用于新诊断癫痫成人患者的单药治疗以及部分性癫痫治疗的辅助治疗。我们的目的是评估急性和重复给予ESL对反射性听源性癫痫发作的有效性和安全性,这通过来自萨拉曼卡的遗传性听源性癫痫发作仓鼠(GASH/Sal)得以体现。动物接受ESL腹腔注射,急性研究采用100、150和200mg/kg的剂量,而亚慢性研究选择100mg/kg的每日剂量,持续14天。在两项研究中,使用神经行为学方法评估治疗的抗惊厥作用。为评估治疗的安全性,进行了行为测试,获取了血液学和生化肝脏指标,并监测了体重。此外,在给予200mg/kg剂量急性给药后测量了血液中的ESL水平。ESL治疗使癫痫发作严重程度降低。在所选剂量之间或药物的急性或重复给药之间未检测到统计学上的显著差异。总之,ESL腹腔注射是安全的,并且在GASH/Sal中显示出抗惊厥作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467e/11117828/606b452f6227/biomedicines-12-01121-g008.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467e/11117828/a6d411805637/biomedicines-12-01121-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467e/11117828/606b452f6227/biomedicines-12-01121-g008.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467e/11117828/e9fd7118d113/biomedicines-12-01121-g002.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467e/11117828/14357b3895ff/biomedicines-12-01121-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467e/11117828/52d5b9078b73/biomedicines-12-01121-g006.jpg
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A Combined Ligand- and Structure-Based Virtual Screening To Identify Novel NaV1.2 Blockers: In Vitro Patch Clamp Validation and In Vivo Anticonvulsant Activity.基于配体和结构的联合虚拟筛选以鉴定新型 NaV1.2 阻滞剂:在体膜片钳验证和体内抗惊厥活性。
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