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- Title
Effects of rosiglitazone, an antidiabetic drug, on Kv3.1 channels.
- Authors
Hyang Mi Lee; Seong Han Yoon; Min-Gul Kim; Sang June Hahn; Bok Hee Choi
- 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 wholecell 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 rosiglitazonemediated 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.
- Subjects
CHO cell; ROSIGLITAZONE; SODIUM channels; HYPOGLYCEMIC agents; GLYCOSYLATED hemoglobin; METFORMIN; SITAGLIPTIN
- Publication
Korean Journal of Physiology & Pharmacology, 2023, Vol 27, Issue 1, p95
- ISSN
1226-4512
- Publication type
Article
- DOI
10.4196/kjpp.2023.27.1.95