Tetrahydroacridine inhibits voltage-dependent Na+ current in guinea-pig ventricular myocytes
文献类型：期刊论文
| 作者 | Wang, W; Wang, YP ; Hu, GY
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2004-09 |
| 卷号 | 25期号:9页码:1138-1144 |
| 关键词 | Alzheimer disease cholinesterase inhibitors sodium channels tetrahydroacridine (tacrine) myocardium patch-clamp techniques |
| ISSN号 | 1671-4083 |
| 文献子类 | Article |
| 英文摘要 | AIM: To study the effects of tetrahydroacridine (tacrine) on voltage-gated Na+ channels in cardiac tissues. METHODS: Single ventricular myocytes were enzymatically-dissociated from adult guinea-pig heart. Voltage-dependent Na+ current was recorded using whole cell voltage-clamp technique. RESULTS: (1) Tacrine reversibly inhibited Na+ current with an IC50 value of 120 mumol/L (95% confidence range: 108-133 mumol/L). (2) The inhibitory effects of tacrine on Na+ current exhibited both a tonic nature and use-dependence. (3) Tacrine at 100 mumol/L caused a negative shift (about 10 mV) in the voltage-dependence of steady-state inactivation of Na+ current, and retarded its recovery from inactivation, but did not affect its activation curve. (4) Intracellular application of tacrine significantly inhibited Na+ current. CONCLUSION: In addition to blocking other voltage-gated ion channels, tacrine blocked Na+ channels in guinea-pig ventricular myocytes. Tacrine acted as inactivation stabilizer of Na+ channels in cardiac tissues. |
| WOS关键词 | RABBIT SINOATRIAL NODE ; 9-AMINO-1,2,3,4-TETRAHYDROACRIDINE THA ; POTASSIUM CURRENT ; HIPPOCAMPAL-NEURONS ; SODIUM-CHANNELS ; TETRAHYDROAMINOACRIDINE ; TACRINE ; RAT ; AXONS ; BLOCK |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000223900000006 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274022]  |
| 专题 | 药理学第二研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Hu, GY |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Dept Pharmacol 1, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, W,Wang, YP,Hu, GY. Tetrahydroacridine inhibits voltage-dependent Na+ current in guinea-pig ventricular myocytes[J]. ACTA PHARMACOLOGICA SINICA,2004,25(9):1138-1144. |
| APA | Wang, W,Wang, YP,&Hu, GY.(2004).Tetrahydroacridine inhibits voltage-dependent Na+ current in guinea-pig ventricular myocytes.ACTA PHARMACOLOGICA SINICA,25(9),1138-1144. |
| MLA | Wang, W,et al."Tetrahydroacridine inhibits voltage-dependent Na+ current in guinea-pig ventricular myocytes".ACTA PHARMACOLOGICA SINICA 25.9(2004):1138-1144. |
入库方式： OAI收割
来源：上海药物研究所
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