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Maprotiline block of the human ether-a-go-go-related gene (HERG) K+ channel.
Author: ChoeHan, ChongSeon Ha, HongHee-Kyung, JoSu-Hyun, JungSung Jun, KohYoung-Sang, YunJi-Hyun
Original Abstract of the Article :
Maprotiline, an atypical antidepressant, can induce prolonged QT and torsades de pointes. We studied the effects of maprotiline on human ether-a-go-go-related gene (HERG) channels expressed in Xenopus oocytes and HEK293 cells. Maprotiline induced a concentration-dependent decrease in current amplitu...See full text at original site
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引用元:
https://doi.org/10.1007/BF02980219
データ提供:米国国立医学図書館(NLM)
Maprotiline's Impact on Heart Rhythm: A Study of HERG Channels
In the realm of [cardiology], the intricate dance of heart rhythm is a delicate balance. This study delves into the effects of maprotiline, an atypical antidepressant, on [HERG channels], which play a crucial role in maintaining this rhythm. Researchers employed a meticulous approach, examining the impact of maprotiline on HERG channels expressed in both [Xenopus oocytes] and [HEK293 cells]. Their findings paint a compelling picture of maprotiline's influence on HERG channel function, revealing a concentration-dependent decrease in current amplitudes and tail currents. This suggests that maprotiline can disrupt the normal electrical activity of the heart, potentially leading to [arrhythmias].
Unveiling the Mechanism: Maprotiline's Interaction with HERG Channels
This study sheds light on the mechanism by which maprotiline disrupts heart rhythm. The researchers found that maprotiline's blockade of HERG channels is not significantly affected by depolarization, suggesting a consistent impact across a range of electrical conditions. Further investigations using [TNBS], an amino-group reagent, revealed that maprotiline's action is likely mediated through interactions with positively charged amino groups within HERG channels. These findings provide valuable insights into the molecular basis of maprotiline's arrhythmogenic effects.
A Balancing Act: Antidepressant Benefits vs. Cardiac Risks
Maprotiline, while effective in managing [depression], poses potential cardiac risks due to its interaction with HERG channels. This research underscores the importance of carefully considering the potential side effects of medications, especially those that affect heart rhythm. Clinicians must carefully weigh the benefits of maprotiline against these risks, especially in patients with pre-existing cardiac conditions.
Dr.Camel's Conclusion
Just like a camel navigating a vast desert, maprotiline, while offering a path to recovery from mental aridity, carries its own risks. This research provides a valuable oasis of knowledge, reminding us of the delicate balance between medication benefits and potential side effects. Understanding the nuances of maprotiline's impact on heart rhythm is crucial for making informed decisions about treatment, ensuring the well-being of those seeking relief from depression.
Date :
- Date Completed 2007-05-29
- Date Revised 2019-09-17
Further Info :
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