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- W4313140596 abstract "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." @default.
- W4313140596 created "2023-01-06" @default.
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- W4313140596 date "1993-06-30" @default.
- W4313140596 modified "2023-10-03" @default.
- W4313140596 title "Effects of rosiglitazone, an antidiabetic drug, on Kv3.1 channels" @default.
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- W4313140596 doi "https://doi.org/10.4196/kjpp.2023.27.1.95" @default.
- W4313140596 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36575937" @default.
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