Pi(4,5)P2 Modulates Hysteresis and Pharmacology of KV7 Channels
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DOI: 10.1016/j.bpj.2016.11.624
Abstract: KV7 channels are critical components of the plasma membrane in many excitable cells. The main function of KV7 channels is to contribute to the maintenance of the resting potential, thus regulating cellular electrical excitability. In… read more here.
Keywords: kv7 kv7; kv7; pharmacology; hysteretic behavior ... See more keywords
Spinal Actions of the NSAID Diclofenac on Nociceptive Transmission in Comparison to the Kv7 Channel Opener Flupirtine
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DOI: 10.1016/j.neuroscience.2020.05.052
Abstract: NSAIDs are the drugs most commonly used to alleviate pain. Despite being a heterogeneous group of compounds, all of them share a mechanism of action based on blockade of COXs enzymes, which confers them anti-inflammatory… read more here.
Keywords: channel; kv7 channels; kv7 channel; activity ... See more keywords
A benzodiazepine activator locks Kv7.1 channels open by electro-mechanical uncoupling.
Sign Up to like & getrecommendations! Published in 2022 at "Communications biology"
DOI: 10.1038/s42003-022-03229-8
Abstract: Loss-of-function mutations in Kv7.1 often lead to long QT syndrome (LQTS), a cardiac repolarization disorder associated with arrhythmia and subsequent sudden cardiac death. The discovery of agonistic IKs modulators may offer a new potential strategy… read more here.
Keywords: kv7 channels; benzodiazepine activator; activator locks; locks kv7 ... See more keywords
Inactivation gating of Kv7.1 channels does not involve concerted cooperative subunit interactions
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DOI: 10.1080/19336950.2018.1441649
Abstract: ABSTRACT Inactivation is an intrinsic property of numerous voltage-gated K+ (Kv) channels and can occur by N-type or/and C-type mechanisms. N-type inactivation is a fast, voltage independent process, coupled to activation, with each inactivation particle… read more here.
Keywords: inactivation gating; process; inactivation; kv7 channels ... See more keywords
Activation of Kv7 channels as a novel mechanism for NO/cGMP‐induced pulmonary vasodilation
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DOI: 10.1111/bph.14662
Abstract: The NO/cGMP pathway represents a major physiological signalling controlling tone in pulmonary arteries (PA), and drugs activating this pathway are used to treat pulmonary arterial hypertension. Kv channels expressed in PA smooth muscle cells (PASMCs)… read more here.
Keywords: novel mechanism; channels novel; cgmp; kv7 channels ... See more keywords
Marked oestrous cycle‐dependent regulation of rat arterial KV7.4 channels driven by GPER1
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DOI: 10.1111/bph.15947
Abstract: Kcnq‐encoded KV7 channels (termed KV7.1–5) regulate vascular smooth muscle cell (VSMC) contractility at rest and as targets of receptor‐mediated responses. However, the current data are mostly derived from males. Considering the known effects of sex,… read more here.
Keywords: marked oestrous; kv7 channels; cycle dependent; oestrous cycle ... See more keywords
A triple cysteine motif as major determinant of the modulation of neuronal KV7 channels by the paracetamol metabolite N‐acetyl‐p‐benzo quinone imine
Sign Up to like & getrecommendations! Published in 2024 at "British Journal of Pharmacology"
DOI: 10.1111/bph.16380
Abstract: The analgesic action of paracetamol involves KV7 channels, and its metabolite N‐acetyl‐p‐benzo quinone imine (NAPQI), a cysteine modifying reagent, was shown to increase currents through such channels in nociceptors. Modification of cysteine residues by N‐ethylmaleimide,… read more here.
Keywords: quinone imine; acetyl benzo; kv7 channels; metabolite acetyl ... See more keywords
Inhibition of Kv7/M Channel Currents by Fangchinoline
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DOI: 10.1159/000527464
Abstract: Introduction: Voltage-gated Kv7/M potassium channels play an essential role in the control of membrane potential and neuronal excitability. Fangchinoline, a bisbenzylisoquinoline alkaloid, displays extensive biological activities including antitumor, anti-inflammatory, and antihypertension effects. In this study,… read more here.
Keywords: channel currents; kv7; kv7 channels; kv7 channel ... See more keywords
Analgesic Action of Acetaminophen via Kv7 Channels
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DOI: 10.3390/ijms24010650
Abstract: The mechanism of acetaminophen (APAP) analgesia is at least partially unknown. Previously, we showed that the APAP metabolite N-acetyl-p-benzoquinone imine (NAPQI) activated Kv7 channels in neurons in vitro, and this activation of Kv7 channels dampened… read more here.
Keywords: kv7; effect; apap; kv7 channels ... See more keywords
Cannabidiol activates neuronal Kv7 channels
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DOI: 10.7554/elife.73246
Abstract: Cannabidiol (CBD), a chemical found in the Cannabis sativa plant, is a clinically effective antiepileptic drug whose mechanism of action is unknown. Using a fluorescence-based thallium flux assay, we performed a large-scale screen and found… read more here.
Keywords: neuronal kv7; cannabidiol activates; kv7; activates neuronal ... See more keywords