Effects of rosiglitazone, an antidiabetic drug, on Kv3.1 channels

• 영문명: Effects of rosiglitazone, an antidiabetic drug, on Kv3.1 channels
• 발행기관: 대한생리학회-대한약리학회
• 저자명: Hyang Mi Lee Seong Han Yoon Min-Gul Kim Sang June Hahn Bok Hee Choi
• 간행물 정보: 『The Korean Journal of Physiology & Pharmacology』제27권 제1호, 95~103쪽, 전체 9쪽
• 주제분류: 의약학 > 의학일반
• 파일형태: PDF
• 발행일자: 2023.01.31

영문 초록

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.

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REFERENCES

키워드

Open channel block Potassium channels Rosiglitazone Shaw-type potassium channels