Properties of voltage-gated Na+ channels in the human rhabdomyosarcoma cell-line SJ-RH30: conventional and automated patch clamp analysis.

作者: A RANDALL , N MCNAUGHTON , P GREEN

DOI: 10.1016/J.PHRS.2006.03.005

关键词:

摘要: Abstract Conventional and automated patch clamp electrophysiology were used to characterise the Na + current of SJ-RH30 human rhabdomyosarcoma. In conventional recordings cells exhibited a fast activating, inactivating at potentials positive −40 mV; in full current–voltage curves maximum occurred between −20 −10 mV. Inactivation kinetics 0 mV biexponential with time constants 0.5 3.7 ms. Deinactivation −90 mV also two kinetic components. Tetrodotoxin (TTX) blocked completely 1 μM. The V 1.4 selective toxin μ-CTx-GIIIB reversibly ∼60% 10 μM. Very similar biophysical behaviour was observed recordings. For example, inactivation mid-point −72 ± 2 mV (slope factor 7.2 ± 0.2) −74 ± 2 mV 7.4 ± 0.4) recording. corresponding values for activation −33.2 ± 2.4 −30.3 ± 2.7 mV 5.8 ± 0.3 6.4 ± 0.3, respectively). throughput method generate additional pharmacological data on inhibition current. TTX inhibited an IC 50 23 nM. channel concentration-dependent manner. Inhibition produced by both tetracaine amitriptyline shown be frequency-dependent. Our experiments indicate that arises mainly from channels phenotype like recombinant channels. suitability these suggests they may useful higher studies interaction drugs skeletal muscle

参考文章(34)
Lori L. Isom, β Subunits: Players in Neuronal Hyperexcitability? Sodium Channels and Neuronal Hyperexcitability. ,vol. 241, pp. 124- 143 ,(2002) , 10.1002/0470846682.CH9
Frank H. Yu, Ruth E. Westenbroek, Inmaculada Silos-Santiago, Kimberly A. McCormick, Deborah Lawson, Pei Ge, Holly Ferriera, Jeremiah Lilly, Peter S. DiStefano, William A. Catterall, Todd Scheuer, Rory Curtis, Sodium Channel β4, a New Disulfide-Linked Auxiliary Subunit with Similarity to β2 The Journal of Neuroscience. ,vol. 23, pp. 7577- 7585 ,(2003) , 10.1523/JNEUROSCI.23-20-07577.2003
Josephine Lai, Frank Porreca, John C. Hunter, Michael S. Gold, Voltage-Gated Sodium Channels and Hyperalgesia Annual Review of Pharmacology and Toxicology. ,vol. 44, pp. 371- 397 ,(2004) , 10.1146/ANNUREV.PHARMTOX.44.101802.121627
Oscar Moran, Alessandra Picollo, Franco Conti, Tonic and Phasic Guanidinium Toxin-Block of Skeletal Muscle Na Channels Expressed in Mammalian Cells Biophysical Journal. ,vol. 84, pp. 2999- 3006 ,(2003) , 10.1016/S0006-3495(03)70026-5
T. Pröbstel, R. Rüdel, J. P. Ruppersberg, Hodgkin-Huxley parameters of the sodium channels in human myoballs. Pflügers Archiv: European Journal of Physiology. ,vol. 412, pp. 264- 269 ,(1988) , 10.1007/BF00582507
Huimin Tao, David Santa Ana, António Guia, Mingxian Huang, Joseph Ligutti, George Walker, Khachonesine Sithiphong, Florence Chan, Tao Guoliang, Zoya Zozulya, Steve Saya, Rick Phimmachack, Charles Sie, Julian Yuan, Lei Wu, Jia Xu, Andrea Ghetti, Automated Tight Seal Electrophysiology for Assessing the Potential hERG Liability of Pharmaceutical Compounds Assay and Drug Development Technologies. ,vol. 2, pp. 497- 506 ,(2004) , 10.1089/ADT.2004.2.497
Wei Zheng, Robert H. Spencer, Laszlo Kiss, High throughput assay technologies for ion channel drug discovery. Assay and Drug Development Technologies. ,vol. 2, pp. 543- 552 ,(2004) , 10.1089/ADT.2004.2.543
Michael E. Bräu, Marc Dreimann, Andrea Olschewski, Werner Vogel, Gunter Hempelmann, Effect of drugs used for neuropathic pain management on tetrodotoxin-resistant Na(+) currents in rat sensory neurons Anesthesiology. ,vol. 94, pp. 137- 144 ,(2001) , 10.1097/00000542-200101000-00024
Glenn Merlino, Lee J Helman, Rhabdomyosarcoma--working out the pathways. Oncogene. ,vol. 18, pp. 5340- 5348 ,(1999) , 10.1038/SJ.ONC.1203038