Role of TREK-1 in Health and Disease, Focus on the Central Nervous System

Conclusion and Perspectives Since their cloning 20 years ago, the physiological importance of TREK-1 channels has continued to grow (Figure 3). Today, TREK-1 channels have been shown to be important and their presence is essential in a number of physiopathological processes. Their involvement in these different processes demonstrate the necessity to design pharmacological modulators, activators or inhibitors, of these channels to correct any TREK-1-related dysfunctions. Despites a number of studies and many molecule screenings, only few putative new drugs were identified. The activators belonging to the ML and BL series show interesting results. However, they display lower affinities (in the micromolar range) and they are not specific for TREK-1 channels as they open other K2P channels. TREK-1 openers are needed in pathologies such as ischemia, epilepsy and pain. The challenge is to improve their affinity, specificity and ability to cross the blood-brain barrier. The new ML and BL series of TREK- activators have not yet been tested in pathologies such epilepsy and ischemia. It would be interesting to investigate any neuroprotection effects of these molecules in rodent models of epilepsy or ischemia. In the same time, their specificity should be improved to avoid any off-target effects resulting from modulating other K2P channels. As inhibitors, the most promising molecules are spadin and its analogs. These peptides are very specific in the K2P family and display very high ...
Source: Frontiers in Pharmacology - Category: Drugs & Pharmacology Source Type: research

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