SKF83959 is a novel triple reuptake inhibitor that elicits anti-depressant activity
文献类型：期刊论文
| 作者 | Fang, Xing1,2; Guo, Lin1,2; Jia, Jia3; Jin, Guo-zhang1,2 ; Zhao, Bin4; Zheng, Yong-yong5; Li, Jian-qi5; Zhang, Ao1,2; Zhen, Xue-chu1,2,3
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| 刊名 | ACTA PHARMACOLOGICA SINICA
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| 出版日期 | 2013-09 |
| 卷号 | 34期号:9页码:1149-1155 |
| 关键词 | SKF83959 monoamine transporter serotonin norepinephrine dopamine depression DOV21947 |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2013.66 |
| 文献子类 | Article |
| 英文摘要 | Aim: SKF83959 (3-methyl-6-chloro-7,8-hydroxy-1-(3-methylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine) is an atypical dopamine receptor-1 (D1 receptor) agonist, which exhibits many D1 receptor-independent effects. In the present work, we examined the effects of SKF83959 on monoaminergic transporters in vitro and its anti-depressant activity in vivo. Methods: Human serotonin transporter (SERT), norepinephrine transporters (NET) or dopamine transporters (DAT) were stably expressed in CHO cells. The uptake kinetics of SERT, NET, and DAT were examined using [H-3]-serotonin, [H-3]-norepinephrine or [H-3]-dopamine, respectively. A triple reuptake inhibitor DOV21947 was used as the positive control. Tail suspension test and forced swimming test were conducted in mice. SKF83959 or DOV21947 (2-8 mg/kg) were intraperitoneally injected 30 min before the tests. Results: SKF83959 was a competitive inhibitor of SERT (K-i=1.43+/-0.45 mu mol/L), but a noncompetitive inhibitor of NET (K-i=0.60+/-0.07 mu mol/L) and DAT (K-i=9.01+/-0.80 mu mol/L). In contrast, DOV21947 was a competitive inhibitor of SERT (K-i=0.89+/-0.24 mu mol/L) and DAT (K-i=1.47+/-0.31 mu mol/L) and a noncompetitive inhibitor of NET (K-i=0.18+/-0.04 mu mol/L). In mice, both SKF83959 and DOV21947 elicited anti-depressant activity in a dose-dependent manner. Conclusion: SKF83959 functions as a novel triple reuptake inhibitor in vitro and exerts anti-depressant effects in vivo. |
| WOS关键词 | DOPAMINE-RECEPTOR ; SKF 83959 ; PARKINSONS-DISEASE ; D1-LIKE RECEPTORS ; IN-VITRO ; RAT ; ANTAGONIST ; MODEL ; PHARMACOLOGY ; ACTIVATION |
| 资助项目 | National Natural Science Foundation of China[81130023] ; National Natural Science Foundation of China[81100918] ; National Natural Science Foundation of China[81271214] ; National Basic Research Plan (973) of the Ministry of Science and Technology of China[2009CB522000] ; National Basic Research Plan (973) of the Ministry of Science and Technology of China[2011CB5C4403] ; Priority Academic Program Development of Jiangsu Higher Education Institutes (PAPD)[00000000] ; Jiangsu Science and Technology Commission[BY2011131] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:4921441 |
| WOS记录号 | WOS:000324170400004 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277475]  |
| 专题 | 药理学第二研究室 |
| 通讯作者 | Guo, Lin |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Synthet Organ & Med Chem Lab, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Dept Pharmacol 2, Shanghai 201203, Peoples R China; 3.Soochow Univ, Coll Pharmaceut Sci, Dept Pharmacol, Suzhou 215123, Peoples R China; 4.Guangdong Med Coll, Affiliated Hosp, Dept Neurol, Zhanjiang 524001, Peoples R China; 5.Shanghai Inst Pharmaceut Ind, Novel Technol Ctr Pharmaceut Chem, Shanghai 200437, Peoples R China |
| 推荐引用方式 GB/T 7714 | Fang, Xing,Guo, Lin,Jia, Jia,et al. SKF83959 is a novel triple reuptake inhibitor that elicits anti-depressant activity[J]. ACTA PHARMACOLOGICA SINICA,2013,34(9):1149-1155. |
| APA | Fang, Xing.,Guo, Lin.,Jia, Jia.,Jin, Guo-zhang.,Zhao, Bin.,...&Zhen, Xue-chu.(2013).SKF83959 is a novel triple reuptake inhibitor that elicits anti-depressant activity.ACTA PHARMACOLOGICA SINICA,34(9),1149-1155. |
| MLA | Fang, Xing,et al."SKF83959 is a novel triple reuptake inhibitor that elicits anti-depressant activity".ACTA PHARMACOLOGICA SINICA 34.9(2013):1149-1155. |
入库方式： OAI收割
来源：上海药物研究所
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