Abstract
TREK-1 is the most studied background K2P channel. Its main role is to control cell excitability and maintain the membrane potential below the threshold of depolarization. TREK-1 is multi-regulated by a variety of physical and chemical stimuli which makes it a very promising and challenging target in the treatment of several pathologies. It is mainly expressed in the brain but also in heart, smooth muscle cells, endocrine pancreas, and prostate. In the nervous system, TREK-1 is involved in many physiological and pathological processes such as depression, neuroprotection, pain, and anesthesia. These properties explain why many laboratories and pharmaceutical companies have been focusing their research on screening and developing highly efficient modulators of TREK-1 channels. In this review, we summarize the different roles of TREK-1 that have been investigated so far in attempt to characterize pharmacological tools and new molecules to modulate cellular functions controlled by TREK-1.
Highlights
In the brain, ion channels regulate a variety of cellular processes such as neurotransmitter release, neuronal excitability, and plasticity
When we look at the brain localization, TREK1 is highly expressed in several regions of the brain such as the olfactory bulb, the hippocampus, the cerebellum and the cortex (Fink et al, 1996)
TREK-1 channels have been shown to be important and their presence is essential in a number of physiopathological processes
Summary
Ion channels regulate a variety of cellular processes such as neurotransmitter release, neuronal excitability, and plasticity. Spadin was the first molecule that was developed in the aim to block TREK-1 channel and mimic the antidepressant-like phenotype of kcnk2−/− mice (Mazella et al, 2010; Djillani et al, 2018). If SSRI antidepressants and antipsychotics drugs act as TREK-1 blockers, mood stabilizers such as lithium chloride and antiepileptics drugs like gabapentine, valproate and carbamazepine were reported to activate TREK-1 channel (Kim et al, 2017).
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