| Tetrahydroacridine inhibits voltage-dependent Na^＋ current in guinea-pig ventricular myocytes |
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| 作者姓名： | Wang W Wang YP Hu GY |
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| 作者单位： | Wei WANG,Yi-ping WANG,Guo-yuan HUState Key Laboratory of Drug Research,The First Department of Pharmacology,Shanghai Institute of Materia Medica,Shanghai Institutes for Biological Sciences,Chinese Academy of Sciences,Shanghai 201203,China |
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| 基金项目： | ProjectsupportedbyagrantfromtheNationalNaturalScienceFoundationofChina(30123005) |
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| 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 120μmol/L(95% confidence range: 108-133μmol/L). (2) The inhibitory effects of tacrine on Na^ current exhibited both a tonic nature and use-dependence. (3) Tacrine at 100μmol/L caused a negative shift (about 10mV) 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.
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| 关 键 词： | 四氢鸭脚木碱 抑制作用 电压 Na^＋ 心室肌细胞 猪 阿尔海默氏疾病 |
Tetrahydroacridine inhibits voltage-dependent Na(+) current in guinea-pig ventricular myocytes |
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| 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. |
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| Authors: | Wang Wei Wang Yi-Ping Hu Guo-Yuan |
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| Institution: | [1]StateKeyLaboratoryofDrugResearch,ShanghaiInstituteofMateriaMedica,ShanghaiInstitutesforBiologicalSciences,ChineseAcademyofSciences,Shanghai201203,China [2]TheFirstDepartmentofPharmacology,ShanghaiInstituteofMateriaMedica,ShanghaiInstitutesforBiologicalSciences,ChineseAcademyofSciences,Shanghai201203,China |
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| Abstract: | 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 umol/L (95 % confidence range: 108-133 umol/L). (2) The inhibitory effects of tacrine on Na current exhibited both a tonic nature and use-dependence. (3) Tacrine at 100 umol/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. |
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| Keywords: | Alzheimer disease cholinesterase inhibitors sodium channels tetrahydroacridine (tacrine) myocardium patch-clamp techniques |
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