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KMID : 0368119940240060889
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Korean Circulation Journal
1994 Volume.24 No. 6 p.889 ~ p.898
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Activation of the Cardiac ATP-Sensitive K+ Channel by KR-30816, a Newly Synthesized Potassium Channel Opener
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Abstract
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Background :
@EN The effects of a newly synthesized potassium channel opener. KR-30816((-)-(nitro-2-hydroxymethyl-2-methyl-2H-l-benzopyran-4-yl) pyridine oxide) on the action potential of papillary muscles of grunea pigs and the ATP-senstive potassium channel
curent(Ikatp) of single ventricular muscele cells of rats were examined to make clear its action mechanism on the KATP channel.
@ES Methods :
@EN We used the conventional microelectrode and the excised inside-out patch configuration.
@ES Results :
@EN KR-30816 caused a shortening of the action potential duration in dose-dependent manner. Wich was inhibited by glibenclamide(3μM). Before run-down of the K+ channel. KR-30816 activated the cardiac ATP-sensitive K+ channel only in the presence
of ATP
and shifted the dose-response relation curve between [ATP] and the channel activity to the right in parallel. After run-down of the KATP channel. KR-30816 did not affect the channel opening either in the absence or in the presence of UDP.
@ES Conclusion : These results suggest that KR-30816 antagonizes the inhibitory effect of ATP on the KATP channel in a competitive manner, thereby enhancing the channel openings.
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