Abstract
The K2P channel TREK-2 is an archetypal polymodal potassium channel which acts to couple a diverse range of regulatory stimuli to cellular electrical excitability. Alongside the other thermo-and mechano-gated K2P channels (TREK-1 and TRAAK) the TREK-2 channel is critical for discrimination of innocuous and noxious temperature and touch sensation. Guided by novel X-ray crystal structures, we have used a variety of electrophysiological, pharmacological and kinetic studies to demonstrate a mechanism of action for the state-dependent inhibition of TREK-2 by norfluoxetine, a biologically active metabolite of the anti-depressant Prozac. These studies also enable us to propose a structural basis for activation of TREK-2 by membrane stretch, temperature and arachidonic acid.
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