traak

RU-TRAAK-2 is a reversible inhibitor of TWIK-related arachidonic acid-stimulated K+ channel with no activity for non-K2P channels including Kv1.2, GIRK2, and Slo1.

2,2,2-Trichloroethanol, the active form of the sedative hypnotic drug chloral hydrate, is an agonist for the nonclassical K2P channels TREK-1 (KCNK2) and TRAAK (KCNK4). It activates a nonclassical potassium channel in cerebrovascular smooth muscle and dilates the middle cerebral artery [1]. [1]. Nikhil K Parelkar, et al. 2,2,2-trichloroethanol Activates a Nonclassical Potassium Channel in Cerebrovascular Smooth Muscle and Dilates the Middle Cerebral Artery. J Pharmacol Exp Ther. 2010 Mar;332(3):803-10.

DCPIB, a known specific and potent inhibitor of volume-regulated anion channels (VRAC),DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1 TRAAK channels.

A1899 is a effective and selective TASK-1 and TASK-3 antagonist.

TREK1 and TREK2 channel activator (EC50 = 0.76 μM in Rb efflux assay in TREK1-expressing CHO cells). Exhibits selectivity for TREK1/2 over TRAAK, TASK3 and a range of other potassium channels. Hyperpolarizes membrane potential of dorsal root ganglion neurons and depresses neuronal activity in vitro. Loucif et al (2018) GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P) channel opener, reduces rat dorsal root ganglion neuron excitability. Br.J.Pharmacol. 175 2272 PMID:29150838

ONO-2920632 is an orally active and CNS-penetrant TREK channel activator with EC50 values of 0.3 µM for TREK-1 and 2.8 µM for TREK-2. It demonstrates selectivity for other K2P channels, showing over 91-fold selectivity against TASK1, TASK2, TASK3, TRAAK, TWIK2, and 31-fold selectivity against TRESK. ONO-2920632 exhibits analgesic effects and is used in the study of pain, migraine, and neurological disorders.