Development of Non-opioid Analgesics Targeting Two-pore Domain Potassium
Channels

Huang, Lu; Xu, Guang–Yin; Jiang, Ruotian; Luo, Yuncheng; Zuo, Yunxia; Liu, Jin

doi:10.2174/1570159x19666210407152528

Cited by 3 publications

(2 citation statements)

References 128 publications

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“…K 2P channels can be regulated by diverse chemical, physical, and metabolic factors, such as extra- or intra-cellular pH, temperature, mechanical stimuli, G proteins, and signaling lipids [ 8 ]. They play an important role in stabilizing resting membrane conductance and repolarizing the action potential of excitable cells [ 9 ].…”

Section: Introductionmentioning

confidence: 99%

Advances in the Understanding of Two-Pore Domain TASK Potassium Channels and Their Potential as Therapeutic Targets

Fan

et al. 2022

Molecules

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TWIK-related acid-sensitive K+ (TASK) channels, including TASK-1, TASK-3, and TASK-5, are important members of the two-pore domain potassium (K2P) channel family. TASK-5 is not functionally expressed in the recombinant system. TASK channels are very sensitive to changes in extracellular pH and are active during all membrane potential periods. They are similar to other K2P channels in that they can create and use background-leaked potassium currents to stabilize resting membrane conductance and repolarize the action potential of excitable cells. TASK channels are expressed in both the nervous system and peripheral tissues, including excitable and non-excitable cells, and are widely engaged in pathophysiological phenomena, such as respiratory stimulation, pulmonary hypertension, arrhythmia, aldosterone secretion, cancers, anesthesia, neurological disorders, glucose homeostasis, and visual sensitivity. Therefore, they are important targets for innovative drug development. In this review, we emphasized the recent advances in our understanding of the biophysical properties, gating profiles, and biological roles of TASK channels. Given the different localization ranges and biologically relevant functions of TASK-1 and TASK-3 channels, the development of compounds that selectively target TASK-1 and TASK-3 channels is also summarized based on data reported in the literature.

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Section: Introductionmentioning

confidence: 99%

Advances in the Understanding of Two-Pore Domain TASK Potassium Channels and Their Potential as Therapeutic Targets

Fan

et al. 2022

Molecules

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“…Besides general anesthesia, this thematic issue also contains some novel perspectives in analgesic pharmacology, particularly based on new ion channels. In the review by Lu Huang et al [ 9 ], the authors fully discuss the advantages and limitations of the translational perspectives of K2P (Two-pore domain potassium) channels in pain medicine and provide outstanding questions for future studies in the end. Besides this article in this thematic issue, another review in the previous issue by Daniel Cook and Peter Goldstein [ 10 ] is also relevant, which summarizes some non-canonical molecular targets for novel analgesics, such as ryanodine receptors (RyRs) and hyperpolarization-activated cyclic nucleotide-gated (HCN) channels.…”

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confidence: 99%