• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

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.

PMID:29201080
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5610745/
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/7ab7/5610745/379ce8c8dff7/ijpr-16-0893-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ab7/5610745/b3af01692d3d/ijpr-16-0893-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ab7/5610745/640d9fdee39f/ijpr-16-0893-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ab7/5610745/0efa871ffb9f/ijpr-16-0893-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ab7/5610745/d82f44e481bc/ijpr-16-0893-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ab7/5610745/379ce8c8dff7/ijpr-16-0893-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ab7/5610745/b3af01692d3d/ijpr-16-0893-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ab7/5610745/640d9fdee39f/ijpr-16-0893-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ab7/5610745/0efa871ffb9f/ijpr-16-0893-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ab7/5610745/d82f44e481bc/ijpr-16-0893-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ab7/5610745/379ce8c8dff7/ijpr-16-0893-g006.jpg

相似文献

1
Anticonvulsant Effects of New 1, 4-DihydropyridineDerivatives Containing Imidazolyl Moiety Against Seizures Induced by Pentylenetetrazole and Maximal Electroshock in Mice.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
Iran J Pharm Res. 2017 Summer;16(3):893-903.
2
Evaluation of anticonvulsant effect of two novels 4-[1-(4-fluorobenzyl)- 5-imidazolyl] dihydropyridine derivatives in mice.两种新型4-[1-(4-氟苄基)-5-咪唑基]二氢吡啶衍生物对小鼠抗惊厥作用的评价。
Res Pharm Sci. 2013 Apr;8(2):91-5.
3
Synthesis and anticonvulsant activity of novel purine derivatives.新型嘌呤衍生物的合成及抗惊厥活性。
Eur J Med Chem. 2014 Sep 12;84:574-83. doi: 10.1016/j.ejmech.2014.07.074. Epub 2014 Jul 22.
4
UPLC-TOF-MS analysis of Galium spurium towards its neuroprotective and anticonvulsant activities.UPLC-TOF-MS 分析拉拉藤对其神经保护和抗惊厥活性的影响。
J Ethnopharmacol. 2012 May 7;141(1):220-7. doi: 10.1016/j.jep.2012.01.056. Epub 2012 Feb 18.
5
Design, synthesis, anticonvulsant, and antiarrhythmic properties of novel N-Mannich base and amide derivatives of β-tetralinohydantoin.新型β-四氢萘乙内酰脲的N-曼尼希碱和酰胺衍生物的设计、合成、抗惊厥及抗心律失常特性
Pharmacol Rep. 2016 Oct;68(5):886-93. doi: 10.1016/j.pharep.2016.04.018. Epub 2016 May 21.
6
Early preclinical evaluation of dihydropyrimidin(thi)ones as potential anticonvulsant drug candidates.二氢嘧啶(硫)酮作为潜在抗惊厥药物候选物的早期临床前评估。
Eur J Pharm Sci. 2017 May 1;102:264-274. doi: 10.1016/j.ejps.2017.03.014. Epub 2017 Mar 15.
7
Synthesis and anticonvulsant activity evaluation of 6-substituted-[1,2,4]triazolo[3,4-a](tetrazolo[5,1-a])phthalazine derivatives.6-取代-[1,2,4]三唑并[3,4-a](四唑并[5,1-a])酞嗪衍生物的合成及抗惊厥活性评价。
J Enzyme Inhib Med Chem. 2013 Aug;28(4):792-800. doi: 10.3109/14756366.2012.684052. Epub 2012 Sep 20.
8
Design, synthesis and pharmacological evaluation of N-[4-(4-(alkyl/aryl/heteroaryl)-piperazin-1-yl)-phenyl]-carbamic acid ethyl ester derivatives as novel anticonvulsant agents.N-[4-(4-(烷基/芳基/杂芳基)-哌嗪-1-基)-苯基]-氨基甲酸乙酯衍生物作为新型抗惊厥剂的设计、合成及药理评价
Bioorg Med Chem Lett. 2015 Mar 1;25(5):1092-9. doi: 10.1016/j.bmcl.2015.01.004. Epub 2015 Jan 9.
9
Design and Synthesis of 5-Substituted Benzo[d][1,3]dioxole Derivatives as Potent Anticonvulsant Agents.5-取代苯并[d][1,3]二氧杂环戊烯衍生物作为强效抗惊厥剂的设计与合成
Arch Pharm (Weinheim). 2017 Feb;350(2). doi: 10.1002/ardp.201600274. Epub 2017 Jan 16.
10
In silico Screening and Evaluation of the Anticonvulsant Activity of Docosahexaenoic Acid-Like Molecules in Experimental Models of Seizures.二十二碳六烯酸样分子在癫痫实验模型中抗惊厥活性的计算机模拟筛选与评价
Iran Biomed J. 2017 Jan;21(1):32-9. doi: 10.6091/.21.1.32. Epub 2016 Sep 4.

本文引用的文献

1
Design, Synthesis and Anti-Tubercular Activity of Novel 1, 4-Dihydropyrine-3, 5-Dicarboxamide Containing 4(5)-Chloro-2-Ethyl- 5(4)-Imidazolyl Moiety.含4(5)-氯-2-乙基-5(4)-咪唑基部分的新型1,4-二氢吡啶-3,5-二甲酰胺的设计、合成及抗结核活性
Iran J Pharm Res. 2016 Fall;15(4):791-799.
2
Design, Synthesis and Evaluation of Antitubercular Activity of Novel Dihydropyridine Containing Imidazolyl Substituent.含咪唑基取代基的新型二氢吡啶的抗结核活性设计、合成与评价
Iran J Pharm Res. 2015 Fall;14(4):1067-75.
3
Docking studies of phthalimide pharmacophore as a sodium channel blocker.
作为钠通道阻滞剂的邻苯二甲酰亚胺药效团的对接研究。
Iran J Basic Med Sci. 2013 Sep;16(9):1016-21.
4
Evaluation of anticonvulsant effect of two novels 4-[1-(4-fluorobenzyl)- 5-imidazolyl] dihydropyridine derivatives in mice.两种新型4-[1-(4-氟苄基)-5-咪唑基]二氢吡啶衍生物对小鼠抗惊厥作用的评价。
Res Pharm Sci. 2013 Apr;8(2):91-5.
5
In vivo pharmacological effects of JZP-4, a novel anticonvulsant, in models for anticonvulsant, antimania and antidepressant activity.新型抗惊厥药物JZP-4在抗惊厥、抗躁狂和抗抑郁活性模型中的体内药理作用。
Pharmacol Biochem Behav. 2008 Jun;89(4):523-34. doi: 10.1016/j.pbb.2008.02.007. Epub 2008 Feb 11.
6
Design, synthesis, and calcium channel antagonist activity of new 1,4-dihydropyridines containing 4-(5)-chloro-2-ethyl-5-(4)-imidazolyl substituent.含4-(5)-氯-2-乙基-5-(4)-咪唑基取代基的新型1,4-二氢吡啶的设计、合成及钙通道拮抗剂活性
Arch Pharm (Weinheim). 2006 Jun;339(6):299-304. doi: 10.1002/ardp.200600013.
7
Synthesis and calcium channel antagonist activity of nifedipine analogues containing 4(5)-chloro-2-methyl-5(4)-imidazolyl substituent.含4(5)-氯-2-甲基-5(4)-咪唑基取代基的硝苯地平类似物的合成及钙通道拮抗剂活性
Boll Chim Farm. 2001 Nov-Dec;140(6):381-6.
8
Anticonvulsant properties of calcium channel blockers in mice: N-methyl-D-,L-aspartate- and Bay K 8644-induced convulsions are potently blocked by the dihydropyridines.钙通道阻滞剂对小鼠的抗惊厥特性:二氢吡啶类药物可有效阻断N-甲基-D-、L-天冬氨酸和Bay K 8644诱导的惊厥。
Epilepsia. 1993 Mar-Apr;34(2):372-80. doi: 10.1111/j.1528-1157.1993.tb02424.x.
9
Suppression of pentylenetetrazole seizures by oral administration of a dihydropyridine Ca2+ antagonist.口服二氢吡啶类钙离子拮抗剂对戊四氮惊厥的抑制作用
Epilepsia. 1987 Jul-Aug;28(4):409-14. doi: 10.1111/j.1528-1157.1987.tb03666.x.
10
Effects of calcium channel inhibitors upon the efficacy of common antiepileptic drugs.钙通道抑制剂对常用抗癫痫药物疗效的影响。
Eur J Pharmacol. 1990 Jan 25;176(1):75-83. doi: 10.1016/0014-2999(90)90134-r.