The Polysite Pharmacology of TREK K2P Channels.
Sign Up to like & getrecommendations! Published in 2021 at "Advances in experimental medicine and biology"
DOI: 10.1007/978-981-16-4254-8_4
Abstract: K2P (KCNK) potassium channels form "background" or "leak" currents that have critical roles in cell excitability control in the brain, cardiovascular system, and somatosensory neurons. Similar to many ion channel families, studies of K2Ps have… read more here.
Keywords: channel; function; trek; polysite pharmacology ... See more keywords
Interaction of cochlin and mechanosensitive channel TREK-1 in trabecular meshwork cells influences the regulation of intraocular pressure
Sign Up to like & getrecommendations! Published in 2017 at "Scientific Reports"
DOI: 10.1038/s41598-017-00430-2
Abstract: In the eye, intraocular pressure (IOP) is tightly regulated and its persistent increase leads to ocular hypertension and glaucoma. We have previously shown that trabecular meshwork (TM) cells might detect aqueous humor fluid shear stress… read more here.
Keywords: intraocular pressure; trabecular meshwork; meshwork cells; trek ... See more keywords
TREK-1 and TREK-2 knockout mice are not resistant to halothane or isoflurane.
Sign Up to like & getrecommendations! Published in 2023 at "Anesthesiology"
DOI: 10.1097/aln.0000000000004577
Abstract: Background: A variety of molecular targets for volatile anesthetics have been suggested, including the anesthetic-sensitive potassium leak channel, TREK-1. Knockout of TREK-1 is reported to render mice resistant to volatile anesthetics, making TREK-1 channels compelling… read more here.
Keywords: minimum alveolar; isoflurane; halothane; trek trek ... See more keywords
Deficiency of TREK‐1 potassium channel exacerbates secondary injury following spinal cord injury in mice
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Neurochemistry"
DOI: 10.1111/jnc.13980
Abstract: Spinal cord injury (SCI) involves complex pathological process which can be complicated by secondary injury. TREK‐1 is a member of the two‐pore domain potassium (K2P) channel family, which can be modulated by a number of… read more here.
Keywords: mice; trek; injury; deficiency ... See more keywords
The two-pore domain potassium channel TREK-1 mediates cardiac fibrosis and diastolic dysfunction
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DOI: 10.1172/jci95945
Abstract: Cardiac two-pore domain potassium channels (K2P) exist in organisms from Drosophila to humans; however, their role in cardiac function is not known. We identified a K2P gene, CG8713 (sandman), in a Drosophila genetic screen and… read more here.
Keywords: dysfunction; two pore; pore domain; domain potassium ... See more keywords
Deficiency of TREK-1 potassium channel exacerbates blood-brain barrier damage and neuroinflammation after intracerebral hemorrhage in mice
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Neuroinflammation"
DOI: 10.1186/s12974-019-1485-5
Abstract: BackgroundIntracerebral hemorrhage (ICH) is a devastating medical emergency with high mortality and severe neurological deficit. ICH-related poor outcomes are due to a combination of pathological processes that could be complicated by secondary insults. TWIK-related K+… read more here.
Keywords: blood brain; intracerebral hemorrhage; hemorrhage; trek ... See more keywords
Sodium permeable and “hypersensitive” TREK‐1 channels cause ventricular tachycardia
Sign Up to like & getrecommendations! Published in 2017 at "EMBO Molecular Medicine"
DOI: 10.15252/emmm.201606690
Abstract: In a patient with right ventricular outflow tract (RVOT) tachycardia, we identified a heterozygous point mutation in the selectivity filter of the stretch‐activated K2P potassium channel TREK‐1 (KCNK2 or K2P2.1). This mutation introduces abnormal sodium… read more here.
Keywords: stretch; sodium permeable; tachycardia; trek ... See more keywords
Shortened Spadin Analogs Display Better TREK-1 Inhibition, In Vivo Stability and Antidepressant Activity
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DOI: 10.3389/fphar.2017.00643
Abstract: Depression is a devastating mental disorder that affects 20% of the population worldwide. Despite their proven efficacy, antidepressants present a delayed onset of action and serious adverse effects. Seven years ago, we described spadin (PE… read more here.
Keywords: antidepressant activity; spadin analogs; trek; stability ... See more keywords
Spadin Selectively Antagonizes Arachidonic Acid Activation of TREK-1 Channels
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DOI: 10.3389/fphar.2020.00434
Abstract: TREK-1 channel activity is a critical regulator of neuronal, cardiac, and smooth muscle physiology and pathology. The antidepressant peptide, spadin, has been proposed to be a TREK-1-specific blocker. Here we sought to examine the mechanism… read more here.
Keywords: trek trek; activation trek; trek; acid ... See more keywords
The Prostacyclin Analogue, Treprostinil, Used in the Treatment of Pulmonary Arterial Hypertension, is a Potent Antagonist of TREK-1 and TREK-2 Potassium Channels
Sign Up to like & getrecommendations! Published in 2021 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2021.705421
Abstract: Pulmonary arterial hypertension (PAH) is an aggressive vascular remodeling disease that carries a high morbidity and mortality rate. Treprostinil (Remodulin) is a stable prostacyclin analogue with potent vasodilatory and anti-proliferative activity, approved by the FDA… read more here.
Keywords: trek trek; arterial hypertension; treatment; pulmonary arterial ... See more keywords
Two-Pore-Domain Potassium Channel TREK–1 Mediates Pulmonary Fibrosis through Macrophage M2 Polarization and by Direct Promotion of Fibroblast Differentiation
Sign Up to like & getrecommendations! Published in 2023 at "Biomedicines"
DOI: 10.3390/biomedicines11051279
Abstract: Idiopathic pulmonary fibrosis (IPF) is a devastating disease characterized by myofibroblast proliferation and abnormal accumulation of extracellular matrix in the lungs. After lung injury, M2 macrophages mediate the pathogenesis of pulmonary fibrosis by secreting fibrotic… read more here.
Keywords: lung fibrosis; pulmonary fibrosis; potassium channel; fibrosis ... See more keywords