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KMID : 0811720230270010095
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Korean Journal of Physiology & Pharmacology
2023 Volume.27 No. 1 p.95 ~ p.103
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Effects of rosiglitazone, an antidiabetic drug, on Kv3.1 channels
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Lee Hyang-Mi
Yoon Seong-Han
Kim Min-Gul
Hahn Sang-June
Choi Bok-Hee
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Abstract
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Rosiglitazone is a thiazolidinedione-class antidiabetic drug that reduces blood glucose and glycated hemoglobin levels. We here investigated the interaction of rosiglitazone with Kv3.1 expressed in Chinese hamster ovary cells using the whole-cell patch-clamp technique. Rosiglitazone rapidly and reversibly inhibited Kv3.1 currents in a concentration-dependent manner (IC50 = 29.8 μM) and accelerated the decay of Kv3.1 currents without modifying the activation kinetics. The rosiglitazone-mediated inhibition of Kv3.1 channels increased steeply in a sigmoidal pattern over the voltage range of ?20 to +30 mV, whereas it was voltage-independent in the voltage range above +30 mV, where the channels were fully activated. The deactivation of Kv3.1 current, measured along with tail currents, was also slowed by the drug. In addition, the steady-state inactivation curve of Kv3.1 by rosiglitazone shifts to a negative potential without significant change in the slope value. All the results with the use dependence of the rosiglitazone-mediated blockade suggest that rosiglitazone acts on Kv3.1 channels as an open channel blocker.
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KEYWORD
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Open channel block, Potassium channels, Rosiglitazone, Shaw-type potassium channels
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