【摘 要】
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Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor used for the treatment of pain and inflammation.Emerging and accumulating evidence suggests that
【机 构】
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The Key Laboratory of Neural and Vascular Biology,Ministry of Education,Department of Pharmacology
【出 处】
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The 3rd Ion Channel Conference: Ion channels-Structure, Func
论文部分内容阅读
Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor used for the treatment of pain and inflammation.Emerging and accumulating evidence suggests that celecoxib can affect cellular targets other than cyclooxygenase, such as ion channels.In this study, we characterised the effects of celecoxib on Kv7 K+ channels and compared its effects with the well-established Kv7 opener retigabine.A perforated whole-cell patch technique was used to record Kv7 currents expressed in HEK 293 ceils and M-type currents from rat SCG neurons.The Key results are as follows: (1) Celecoxib enhances Kv7.2-7.4, Kv7.2/7.3 and Kv7.3/7.5 currents but inhibits Kv7.1 and Kv7.1/KCNE 1 currents.(2) The effect of celecoxib is concentration dependent.The concentration for the half-maximal effect of celecoxib on inhibition of Kv7.1 (IC50) is approximately 4 μM and on activation of Kv7.2-7.4, Kv7.2/7.3 and Kv7.3/7.5 (EC50S) are approximately 2-5 μM.(3) The effects of celecoxib are manifested by increasing current amplitudes, shifting the voltage-dependent activation curve in a more negative direction and slowing the deactivation of Kv7 currents.
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