Title : Inhibitory effects of SKF96365 on the activities of K(+) channels in mouse small intestinal smooth muscle cells - Tanahashi_2016_J.Vet.Med.Sci_78_203 |
Author(s) : Tanahashi Y , Wang B , Murakami Y , Unno T , Matsuyama H , Nagano H , Komori S |
Ref : J Vet Med Sci , 78 :203 , 2016 |
Abstract :
In order to investigate the effects of SKF96365 (SKF), which is a non-selective cationic channel blocker, on K(+) channel currents, we recorded currents through ATP sensitive K(+) (IKATP), voltage-gated K(+) (IKv) and Ca(2+) activated K(+) channels (IBK) in the absence and presence of SKF in single small intestinal myocytes of mice with patch-clamp techniques. SKF (10 microM) reversibly abolished IKATP that was induced by cromakalim (10 microM), which is a selective ATP sensitive K(+) channel opener. These inhibitory effects were induced in a concentration-dependent and voltage-independent manner. The 50% inhibitory concentration (IC50) was 0.85 microM, which was obviously lower than that reported for the muscarinic cationic current. In addition, SKF (1 microM approximately the IC50 value in IKATP suppression) reversibly inhibited the IKv that was induced by repetitive depolarizing pulses from -80 to 20 mV. However, the extent of the inhibitory effects was only ~30%. In contrast, SKF (1 microM) had no significant effects on spontaneous transient IBK and caffeine-induced IBK. These results indicated that SKF inhibited ATP sensitive K(+) channels and voltage-gated K(+) channels, with the ATP sensitive K(+) channels being more sensitive than the voltage-gated K(+) channels. These inhibitory effects on K(+) channels should be considered when SKF is used as a cationic channel blocker. |
PubMedSearch : Tanahashi_2016_J.Vet.Med.Sci_78_203 |
PubMedID: 26498720 |
Tanahashi Y, Wang B, Murakami Y, Unno T, Matsuyama H, Nagano H, Komori S (2016)
Inhibitory effects of SKF96365 on the activities of K(+) channels in mouse small intestinal smooth muscle cells
J Vet Med Sci
78 :203
Tanahashi Y, Wang B, Murakami Y, Unno T, Matsuyama H, Nagano H, Komori S (2016)
J Vet Med Sci
78 :203