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| Title: | β1-SELECTIVE ANTAGONISTS ARE MORE EFFECTIVE FOR THE TREATMENT OF TYPE 1 LONG QT SYNDROME | |
| DOI No: | 10.1142/9789812702234_0073 | |
| Source: | ADVANCES IN ELECTROCARDIOLOGY 2004 (pp 274-277) | |
| Author(s): | KAZUNOBU KAWAKAMI
The Second Department of Internal Medicine, University of Occupational and Environmental Health, Japan 1-1 Iseigaoka, Yahatanishi-ku, Kitakyusyu, 807-0855, Japan TOSHIHISA NAGATOMO The Second Department of Internal Medicine, University of Occupational and Environmental Health, Japan 1-1 Iseigaoka, Yahatanishi-ku, Kitakyusyu, 807-0855, Japan HARUHIKO ABE The Second Department of Internal Medicine, University of Occupational and Environmental Health, Japan 1-1 Iseigaoka, Yahatanishi-ku, Kitakyusyu, 807-0855, Japan YASUSHI OGINOSAWA The Second Department of Internal Medicine, University of Occupational and Environmental Health, Japan 1-1 Iseigaoka, Yahatanishi-ku, Kitakyusyu, 807-0855, Japan TAKUO TSURUGI The Second Department of Internal Medicine, University of Occupational and Environmental Health, Japan 1-1 Iseigaoka, Yahatanishi-ku, Kitakyusyu, 807-0855, Japan YASUHIDE NAKASHIMA The Second Department of Internal Medicine, University of Occupational and Environmental Health, Japan 1-1 Iseigaoka, Yahatanishi-ku, Kitakyusyu, 807-0855, Japan |
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| Abstract: | Objective: In type 1 of the Long QT syndrome (LQT), arrhythmia attacks are usually recognized when the adrenergic activity is increasing. β-blockers are generally used for the treatment of LQT1 patients to prevent tachyarrhythmia attack. However, some β-blocking agents have also reported to inhibit HERG channels by direct action to the channels. We hypothesized that variation of the effect of β-blockers on HERG channels might be explained by the structure of the drugs based on the β-receptor subtype. Method: HERG channels were stably expressed in HEK293 cells, and the current was recorded by using whole-cell patch-clamp technique. Result: Non-selective β-blockers, propranolol and carvedilol, inhibited the HERG current in a dose-dependant manner (IC50 9.0 μM and 0.74 μM, respectively). β2-selective blocker, ICI 118551, inhibited the HERG current (IC50 9.2 μM) in the same manner as for propranolol, while the β1-selective blocker, atenolol, did not inhibit the HERG current significantly. Conclusion: β-blockers with β2-receptor blocking action inhibited HERG channels expressed in HEK 293 cells. β1-selective blockers may be preferable for the treatment of LQT1 patients, since the HERG channel dependency is increased in the LQT1 patients. | |
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