Chemoselective regulation of TREK2 channel: Activation by sulfonate chalcones and inhibition by sulfonamide chalcones |
| |
| Authors: | Eun-Jin Kim Hyung Won Ryu Marcus J. Curtis-Long Jaehee Han Jun Young Kim Jung Keun Cho Dawon Kang Ki Hun Park |
| |
| Affiliation: | 1. Division of Applied Life Science (BK21 program), EB-NCRC, Institute of Agriculture & Life Science, Graduate School of Gyeongsang National University, Jinju 660-701, Republic of Korea;2. Medical Research Center for Neural Dysfunction, Department of Physiology, School of Medicine, Gyeongsang National University, Jinju 660-751, Republic of Korea;3. 12 New Road, Nafferton, East Yorkshire, YO25 4JP, UK |
| |
| Abstract: | Although it has not been extensively studied, a significant volume of literature suggests that TREK2 will probably turn out to be an important channel in charge of tuning neuronal transmitter and hormone levels. Thus, pharmacological tools which can manipulate this channel, such as selective agonists are essential both in drug design and to further our understanding of this system. Our investigations have shown that sulfonate (‘O’) chalcone and sulfonamide (‘N’) chalcones regulate the TREK2 channel in remarkably different ways: sulfonamide chalcone 5 behaved as an inhibitor with an IC50 of 62 μM, whereas the sulfonate analogue 11 activated TREK2 with EC50 value of 167 μM. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
