Allosteric modulation of sigma-1 receptors elicits anti-seizure activities
文献类型：期刊论文
| 作者 | Guo, Lin1,4; Chen, Yanke1,4; Zhao, Rui1,4; Wang, Guanghui1,4; Friedman, Eitan2; Zhang, Ao3 ; Zhen, Xuechu1,4
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| 刊名 | BRITISH JOURNAL OF PHARMACOLOGY
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| 出版日期 | 2015-08 |
| 卷号 | 172期号:16页码:4052-4065 |
| ISSN号 | 0007-1188 |
| DOI | 10.1111/bph.13195 |
| 文献子类 | Article |
| 英文摘要 | Background and PurposeApplication of orthosteric sigma-1 receptor agonists as anti-seizure drugs has been hindered by questionable efficacy and potential adverse effects. Here, we have investigated the anti-seizure effects of the novel and potent allosteric modulator of sigma-1 receptors, SKF83959 and its derivative SOMCL-668 (3-methyl-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-ol). Experimental ApproachThe anti-seizure effects of SKF83959 were investigated in three mouse models, maximal electroshock seizures, pentylenetetrazole-induced convulsions and kainic acid-induced status epilepticus'. Also, in rats, the cortical epileptiform activity induced by topical application of picrotoxin was recorded in electrocorticograms. In rat hippocampal brain slices, effects of the drugs on the high potassium-evoked epileptiform local field potentials were studied. Anti-seizure activities of SOMCL-668, a newly developed sigma-1 receptor selective allosteric modulator, were also investigated. Key ResultsSKF83959 (20, 40mg |
| WOS关键词 | PROTEIN-COUPLED RECEPTORS ; ANTIEPILEPTIC DRUGS ; ARRIVE GUIDELINES ; DOPAMINE-RECEPTOR ; CONCISE GUIDE ; GUINEA-PIG ; SKF83959 ; PHARMACOLOGY ; RAT ; MICE |
| 资助项目 | National Science Foundation of China[81402905] ; National Science Foundation of China[81130023] ; National Science Foundation of China[30825042] ; National Basic Research Plan (973) of the Ministry of Science and Technology of China[2011CB504403] ; Priority Academic Program Development of Jiangsu Higher Education Institute (PAPD)[00000000] ; Jiangsu Key Laboratory[BM2013003] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000358454100009 |
| 出版者 | WILEY-BLACKWELL |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276457]  |
| 专题 | 药理学第二研究室 药物化学研究室 |
| 通讯作者 | Zhen, Xuechu |
| 作者单位 | 1.Soochow Univ, Coll Pharmaceut Sci, Dept Pharmacol, Suzhou 215123, Jiangsu, Peoples R China; 2.CUNY, Dept Pharmacol & Neurosci, Sch Med CCNY, New York, NY 10021 USA; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, Shanghai 200031, Peoples R China 4.Soochow Univ, Coll Pharmaceut Sci, Jiangsu Key Lab Translat Res & Therapy Neuropsych, Suzhou 215123, Jiangsu, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Guo, Lin,Chen, Yanke,Zhao, Rui,et al. Allosteric modulation of sigma-1 receptors elicits anti-seizure activities[J]. BRITISH JOURNAL OF PHARMACOLOGY,2015,172(16):4052-4065. |
| APA | Guo, Lin.,Chen, Yanke.,Zhao, Rui.,Wang, Guanghui.,Friedman, Eitan.,...&Zhen, Xuechu.(2015).Allosteric modulation of sigma-1 receptors elicits anti-seizure activities.BRITISH JOURNAL OF PHARMACOLOGY,172(16),4052-4065. |
| MLA | Guo, Lin,et al."Allosteric modulation of sigma-1 receptors elicits anti-seizure activities".BRITISH JOURNAL OF PHARMACOLOGY 172.16(2015):4052-4065. |
入库方式： OAI收割
来源：上海药物研究所
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