Kir3 channel signaling complexes: Focus on opioid receptor signaling [PDF]
Frontiers in Cellular Neuroscience, 2014 Opioids are among the most effective drugs to treat severe pain. They produce their analgesic actions by specifically activating opioid receptors located along the pain perception pathway where they inhibit the flow of nociceptive information.
Karim eNagi, Graciela ePineyro
doaj +3 more sources
Kir3 channel ontogeny - the role of Gβγ subunits in channel assembly and trafficking. [PDF]
Frontiers in Cellular Neuroscience, 2014 The role of Gβγ subunits in Kir3 channel gating is well characterized. Here, we have studied the role of Gβγ dimers during their initial contact with Kir3 channels, prior to their insertion into the plasma membrane.
Peter eZylbergold +5 more
doaj +3 more sources
Chronic ethanol exposure in mice evokes pre- and postsynaptic deficits in GABAergic transmission in ventral tegmental area GABA neurons. [PDF]
Br J PharmacolAbstract Background and purpose GABAergic neurons in mouse ventral tegmental area (VTA) exhibit elevated activity during withdrawal following chronic ethanol exposure. While increased glutamatergic input and decreased GABAA receptor sensitivity have been implicated, the impact of inhibitory signaling in VTA GABA neurons has not been fully addressed ...
Mitten EH +5 more
europepmc +2 more sources
Kir3 channel blockade in the cerebellar cortex suppresses performance of classically conditioned Purkinje cell responses. [PDF]
Sci Rep, 2020 AbstractIn the eyeblink conditioning paradigm, cerebellar Purkinje cells learn to respond to the conditional stimulus with an adaptively timed pause in its spontaneous firing. Evidence suggests that the pause is elicited by glutamate released from parallel fibers and acting on metabotropic receptors (mGluR7) which initiates a delayed-onset suppression ...
Johansson F, Hesslow G.
europepmc +4 more sources
Mechanism of PLC-Mediated Kir3 Current Inhibition [PDF]
Channels, 2007 A large number of ion channels maintain their activity through direct interactions with phosphatidylinositol bisphosphate (PIP2). For such channels, hydrolysis of PIP2 causes current inhibition. It has become controversial whether the inhibitory effects on channel activity represent direct effects of PIP2 hydrolysis or of downstream PKC action.
Inna, Keselman +3 more
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Modulation of Neuronal Kir3 Channels by Cholesterol [PDF]
Biophysical Journal, 2016 In recent years, cholesterol emerged as a major regulator of ion channel function. The most common effect of cholesterol on ion channels is a decrease in channel activity. We have recently shown that unexpectedly cholesterol enrichment up-regulates G-protein gated inwardly rectifying potassium (GIRK or Kir3) activity in atrial myocytes.Here we focus on
Bukiya, Anna N. +1 more
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Subunit-Specific Regulation of Kir3 Channels by Sorting nexin 27 [PDF]
Channels, 2007 G protein-gated inwardly rectifying potassium (Kir3) channels are involved in regulating membrane excitability in the brain. Kir3 channels have been shown to play a role in learning, analgesia and drug addiction. Little is known about the cell surface regulation of Kir3 channels. Using a proteomics approach, we recently discovered that sorting nexin 27
Rounak, Nassirpour, Paul A, Slesinger
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Further Structure-Activity Relationship of G Protein-Gated Inwardly Rectifying Potassium Channels 1/2 Activators: Synthesis and Biological Characterization of In Vitro Tool Compounds. [PDF]
ChemMedChemWork presented here details the design and characterize novel G protein‐gated inwardly rectifying potassium channels (GIRK)1/2 activators. A new 4,4‐difluorocyclohexylpyrazole have been identified that confers improved potency and selectivity for GIRK1/2 versus GIRK1/4.
Nahid S +8 more
europepmc +2 more sources
Behavioral characterization of mice lacking GIRK/Kir3 channel subunits [PDF]
Genes, Brain and Behavior, 2008 G protein‐gated inwardly rectifying K+ (GIRK/Kir3) channels mediate the postsynaptic inhibitory effects of many neurotransmitters and drugs of abuse. The lack of drugs selective for GIRK channels has hindered our ability to study their contributions to behavior.
M, Pravetoni, K, Wickman
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Absence and Rescue of Morphine Withdrawal in GIRK/Kir3 Knock-out Mice [PDF]
The Journal of Neuroscience, 2008 Although morphine induces both analgesia and dependence through μ-opioid receptors (MORs), the respective contributions of the intracellular effectors engaged by MORs remain unknown. To examine the contribution of G-protein-gated inwardly rectifying K+(GIRK, Kir3) channels to morphine dependence and analgesia, we quantified naloxone-precipitated ...
Cruz, Joana +6 more
openaire +3 more sources