TWIK-1/TREK-1-IN-1

TWIK-1/TREK-1-IN-1 (compound 2a) is an inhibitor of the TWIK-related potassium channel (Potassium Channel) TREK-1. TREK-1 contains a two-pore domain potassium (K2p) channel that dimerizes into TREK-1 homodimer and TWIK-1/TREK-1 heterodimer, and is an important antidepressant target. TWIK-1/TREK-1-IN-3 targets TREK-1 homodimer and TWIK-1/TREK-1 heterodimer with IC50s of 9.36 μM and 14.6 μM, respectively, and has antidepressant-like effects[1].

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

IC50: 9.36 μM (TREK-1/TREK-1), 14.6 μM (TWIK-1/TREK-1)[1]

[1]. Lee EH, et al. Novel potent blockers for TWIK-1/TREK-1 heterodimers as potential antidepressants. Biomed Pharmacother. 2023 Sep;165:115139.. .