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Description: Sematilide (formerly known as CK-1752) is a novel class III antiarrhythmic agent. It acts as a selective delayed rectifier K+ current (IKr) channel blocker. I The sematilide-sensitive current, which was recorded by means of a triangular voltage command, showed a strong inward rectification and had a peak at about -40 mV, suggesting that sematilide inhibits the rapidly activating delayed rectifier K+ current. The Ca2+-independent transient K+ and the inward rectifier K+ currents were not affected significantly by application of 100 microM sematilide. Moreover, voltage-dependent Na+ and Ca2+ currents were not affected significantly by 100 microM sematilide. These findings indicate that sematilide selectively blocks the rapidly activating delayed rectifier K+ current in atrial myocytes and provide evidence supporting the usefulness of the drug as a class III antiarrhythmic agent.
References: Eur J Pharmacol. 1997 Jul 23; 331(2-3):295-302; Circ J. 2002 Aug; 66(8):758-62.
Related CAS#:101526-83-4 (free base)
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