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Updated: Aug 20, 2026

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
Published on: January 27, 2013
ATP-dependent potassium channels as a key target for the treatment of myocardial and vascular dysfunction
Piero Pollesello1, Alexandre Mebazaa
1Orion-Pharma, Cardiovascular and Critical Care, Espoo, Finland.
Purpose Of Review:
The aim of this review is to highlight the most recent and interesting articles on the physiologic properties and functions of ATP-dependent potassium channels in the cardiovascular system and on the role of the potassium channel openers for the treatment of cardiovascular dysfunction.
Recent Findings:
The initial efforts in the development of potassium channel openers focused on the management of systemic hypertension. Lately, the range of possible indications for potassium channel openers has increased to include pulmonary hypertension and stable angina pectoris. The discovery of a connection between the mitochondrial ATP-dependent potassium channels and the phenomenon of cardiac preconditioning created potential new uses for potassium channel openers in myocardial ischemia, inn unstable angina, in preoperative and perioperative settings, and for the preservation of organs for transplant.
Summary:
The most recent data on the physiologic roles of sarcolemmal and mitochondrial ATP-dependent potassium channels and the pharmacology of potassium channel openers in the cardiovascular system are summarized and discussed. Finally, the effects of potassium channel opener drugs including minoxidil, nicorandil, pinacidil, bimakalin, and levosimendan, a dual-action potassium channel opener and calcium sensitizer with inodilator and cardioprotective activity, are discussed.
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