Results 51 to 60 of about 10,013 (222)

HL-1 cells express an inwardly rectifying K+ current activated via muscarinic receptors comparable to that in mouse atrial myocytes [PDF]

open access: yes, 2010
An inwardly rectifying K^+ current is present in atrial cardiac myocytes that is activated by acetylcholine (I_{KACh}). Physiologically, activation of the current in the SA node is important in slowing the heart rate with increased parasympathetic tone ...
A Benians   +44 more
core   +2 more sources

AsKC11, a Kunitz Peptide from Anemonia sulcata, Is a Novel Activator of G Protein-Coupled Inward-Rectifier Potassium Channels

open access: yesMarine Drugs, 2022
(1) Background: G protein-coupled inward-rectifier potassium (GIRK) channels, especially neuronal GIRK1/2 channels, have been the focus of intense research interest for developing drugs against brain diseases.
Dongchen An   +7 more
doaj   +1 more source

Discovery, characterization and structure-activity relationships of an inhibitor of inward rectifier potassium (Kir) channels with preference for Kir2.3, Kir3.X and Kir7.1

open access: yesFrontiers in Pharmacology, 2011
The inward rectifier family of potassium (Kir) channels is comprised of at least 16 family members exhibiting broad and often overlapping cellular, tissue or organ distributions.
Jerod S Denton
doaj   +1 more source

Sleep-deprivation regulates α-2 adrenergic responses of rat hypocretin/orexin neurons. [PDF]

open access: yesPLoS ONE, 2011
We recently demonstrated, in rat brain slices, that the usual excitation by noradrenaline (NA) of hypocretin/orexin (hcrt/orx) neurons was changed to an inhibition following sleep deprivation (SD).
Aaron Uschakov   +7 more
doaj   +1 more source

Probing the role of the cation–π interaction in the binding sites of GPCRs using unnatural amino acids [PDF]

open access: yes, 2009
We describe a general application of the nonsense suppression methodology for unnatural amino acid incorporation to probe drug–receptor interactions in functional G protein-coupled receptors (GPCRs), evaluating the binding sites of both the M2 muscarinic
Ballesteros   +31 more
core   +3 more sources

G-Protein-Gated Inwardly Rectifying Potassium (Kir3/GIRK) Channels Govern Synaptic Plasticity That Supports Hippocampal-Dependent Cognitive Functions in Male Mice

open access: yesJournal of Neuroscience, 2021
The G-protein-gated inwardly rectifying potassium (Kir3/GIRK) channel is the effector of many G-protein-coupled receptors (GPCRs). Its dysfunction has been linked to the pathophysiology of Down syndrome, Alzheimer's and Parkinson's diseases, psychiatric ...
Souhail Djebari   +9 more
semanticscholar   +1 more source

TRPC4 and GIRK channels underlie neuronal coding of firing patterns that reflect Gq/11–Gi/o coincidence signals of variable strengths

open access: yesProceedings of the National Academy of Sciences of the United States of America, 2022
Significance Neurons communicate by releasing neurotransmitters, many of which act at G protein–coupled receptors. Although it is well known that Gq/11 accelerates action potential firing while Gi/o inhibits firing, how firing patterns change in response
J. Tian   +6 more
semanticscholar   +1 more source

Structural mechanism underlying G protein family-specific regulation of G protein-gated inwardly rectifying potassium channel

open access: yesNature Communications, 2019
Opening of G protein-gated inwardly rectifying potassium channels (GIRK) is coupled to the activation of a GPCR. Here the authors use NMR and cell-based BRET assays to gain insights into the mechanisms underlying family-specific activation and find that ...
Hanaho Kano   +7 more
doaj   +1 more source

Inhibition of G Protein-Activated Inwardly Rectifying K+ Channels by the Antidepressant Paroxetine

open access: yesJournal of Pharmacological Sciences, 2006
Paroxetine is commonly used as a selective serotonin reuptake inhibitor for the treatment of depression and other psychiatric disorders. However, the molecular mechanisms of the paroxetine effects have not yet been sufficiently clarified.
Toru Kobayashi   +2 more
doaj   +1 more source

Gain of function mutants: Ion channels and G protein-coupled receptors [PDF]

open access: yes, 2000
Many ion channels and receptors display striking phenotypes for gain-of-function mutations but milder phenotypes for null mutations. Gain of molecular function can have several mechanistic bases: selectivity changes, gating changes including constitutive
Karschin, Andreas, Lester, Henry A.
core   +1 more source

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