Alosetron and the rapid component of delayed rectifying potassium current in cardiac cells
| Autor: | James L. Kenyon, Kenton M. Sanders, A. Carl |
|---|---|
| Rok vydání: | 2001 |
| Předmět: |
medicine.medical_specialty
Patch-Clamp Techniques Potassium Channels Pyridines Voltage clamp Long QT syndrome Guinea Pigs In Vitro Techniques Pharmacology QT interval General Biochemistry Genetics and Molecular Biology Membrane Potentials Piperidines Internal medicine medicine Animals General Pharmacology Toxicology and Pharmaceutics Cisapride business.industry Myocardium Cardiac muscle Antagonist Heart General Medicine medicine.disease Potassium channel medicine.anatomical_structure Potassium Channels Voltage-Gated Alosetron Receptors Serotonin Cardiology Serotonin Antagonists Receptors Serotonin 5-HT3 business Carbolines Delayed Rectifier Potassium Channels medicine.drug |
| Zdroj: | Life Sciences. 68:1585-1591 |
| ISSN: | 0024-3205 |
| Popis: | Some drugs acting on 5-hydroxytryptamine receptors inhibit the rapid component of delayed rectifying potassium currents (I(Kr)) in cardiac muscle cells. This is associated with lengthening of the QT interval in the cardiac cycle and can lead to fatal arrhythmias. We investigated whether alosetron, a novel 5HT3 antagonist proposed for treatment of irritable bowel syndrome (IBS), blocks I(Kr) in guinea pig cardiac myocytes. I(Kr) was isolated under whole-cell voltage clamp, and was identified by its sensitivity to the selective I(Kr) antagonist E4031. Cisapride (10(-6) M) inhibited the E4031-sensitive current while alosetron (10(-10)-10(-6) M) had no effect on I(Kr). We also found that alosetron did not inhibit I(Ks). Therefore, use of alosetron for treatment of IBS should not be confounded by long QT syndrome. |
| Databáze: | OpenAIRE |
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