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ONO-2920632 is an activator of two-pore domain potassium channel 2.1 (K2P2.1/TREK-1) and K2P10.1/TREK-2.1 It induces K2P2.1/TREK-1 and K2P10.1/TREK-2 activity in thallium flux assays using CHO cells expressing K2P2.1/TREK-1 and HEK293 cells expressing K2P10.1/TREK-2 (EC50s = 2.8 and 0.3 µM, respectively). ONO-2920632 is selective for K2P2.1/TREK-1 and K2P10.1/TREK-2 over 72 other ion channels, G protein-coupled receptors (GPCRs), transporters, and nuclear hormones at 10 µM. In vivo, ONO-2920632 (3 mg/kg) prevents acetic acid-induced writhing in mice.
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1. Discovery of ONO-