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含咪唑基的新型1,4-二氢吡啶衍生物对小鼠戊四氮和最大电休克诱发惊厥的抗惊厥作用

Anticonvulsant Effects of New 1, 4-DihydropyridineDerivatives Containing Imidazolyl Moiety Against Seizures Induced by Pentylenetetrazole and Maximal Electroshock in Mice.

作者信息

Rasouli Yasaman, Davood Asghar, Alaee Armin, Dehqani Golnoush, Shafaroudi Hamed, Lotfinia Mahboubeh, Amini Mohsen, Shafiee Abbas

机构信息

Department of Medicinal Chemistry, Faculty of Pharmacy, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran.

Department of Pharmacology, Faculty of Pharmacy, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran.

出版信息

Iran J Pharm Res. 2017 Summer;16(3):893-903.

Abstract

Epilepsy is a chronic disorder of the brain affecting around 50 million people in the world. Up to 30% of epileptic patients do not respond to available drugs and medical therapies. In this paper, anticonvulsant screening of 10 synthesized new derivatives of 1, 4-dihydropyridine-3, 5-dicarboxamides was performed. Anticonvulsant activity was evaluated by intravenous and intraperitoneal pentylenetetrazole and maximal electroshock induced seizures tests. Nifedipine was used as reference drug. Our pharmacological results revealing the compounds 2, 4, 5, and 6 can be effective in both absence and grandmal seizures in human. These pharmacological studies have displayed that these new dihydropyridine derivatives are capable to inhibiting seizures induced by pentylenetetrazole and maximal electroshock in mice efficiently.

摘要

癫痫是一种慢性脑部疾病,全球约有5000万人受其影响。高达30%的癫痫患者对现有的药物和医学疗法没有反应。本文对10种合成的1,4 - 二氢吡啶 - 3,5 - 二羧酸酰胺新衍生物进行了抗惊厥筛选。通过静脉注射和腹腔注射戊四氮以及最大电休克诱导惊厥试验来评估抗惊厥活性。硝苯地平用作参考药物。我们的药理学结果表明,化合物2、4、5和6对人类失神发作和大发作均可能有效。这些药理学研究表明,这些新的二氢吡啶衍生物能够有效抑制小鼠中由戊四氮和最大电休克诱导的惊厥。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ab7/5610745/b3af01692d3d/ijpr-16-0893-g002.jpg

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