Results 11 to 20 of about 5,036 (195)

Gi/o-coupled muscarinic receptors co-localize with GIRK channel for efficient channel activation. [PDF]

open access: yesPLoS ONE, 2018
G protein-gated inwardly rectifying K+ (GIRK) channel regulates cellular excitability upon activation of Gi/o-coupled receptors. In Gi/o-coupled muscarinic M2R, the intracellular third loop (i3) is known as a key domain for Gi/o coupling, because ...
Michihiro Tateyama, Yoshihiro Kubo
doaj   +2 more sources

Pharmacological Characterization of 5-HT1A Autoreceptor-Coupled GIRK Channels in Rat Dorsal Raphe 5-HT Neurons.

open access: yesPLoS ONE, 2015
G protein-activated inwardly rectifying potassium (GIRK) channels in 5-HT neurons are assumed to be principal effectors of 5-hydroxytryptamine 1A (5-HT1A) autoreceptors, but their pharmacology, subunit composition and the role in regulation of 5-HT ...
Alberto Montalbano   +2 more
doaj   +2 more sources

Increased GIRK channel activity prevents arrhythmia in mice with heart failure by enhancing ventricular repolarization

open access: yesScientific Reports, 2023
Ventricular arrhythmia causing sudden cardiac death is the leading mode of death in patients with heart failure. Yet, the mechanisms that prevent ventricular arrhythmias in heart failure are not well characterized.
Xue An, Hana Cho
doaj   +2 more sources

Atrial GIRK Channels Mediate the Effects of Vagus Nerve Stimulation on Heart Rate Dynamics and Arrhythmogenesis [PDF]

open access: yesFrontiers in Physiology, 2018
Diminished parasympathetic influence is central to the pathogenesis of cardiovascular diseases, including heart failure and hypertension. Stimulation of the vagus nerve has shown promise in treating cardiovascular disease, prompting renewed interest in ...
Steven W. Lee   +5 more
doaj   +2 more sources

Identification of a G-Protein-Independent Activator of GIRK Channels

open access: yesCell Reports, 2020
Summary: G-protein-gated inwardly rectifying K+ (GIRK) channels are essential effectors of inhibitory neurotransmission in the brain. GIRK channels have been implicated in diseases with abnormal neuronal excitability, including epilepsy and addiction ...
Yulin Zhao   +10 more
doaj   +3 more sources

Optical control of GIRK channels using visible light

open access: yesOrganic & Biomolecular Chemistry, 2017
We have developed the photoswitchable GIRK channel agonist VLOGO , which permits the precise control of GIRK channels using visible light.
Trads, Julie B   +8 more
openaire   +4 more sources

(+)-Trans-Cannabidiol Is an Agonist at Human CB<sub>2</sub> Receptors. [PDF]

open access: yesPharmacol Res Perspect
ABSTRACT (−)‐trans‐Cannabidiol ((−)‐CBD) is a principal phytocannabinoid from Cannabis sativa. (−)‐CBD has complex pharmacology but is a relatively weak inhibitor of CB1 and CB2 receptor signaling. Cannabidiol has two chiral centres and thus four stereoisomers.
Burtchaell PB   +6 more
europepmc   +2 more sources

Comparing CB1 receptor GIRK channel responses to receptor internalization using a kinetic imaging assay

open access: yesScientific Reports
The type 1 cannabinoid receptor (CB1R) mediates neurotransmitter release and synaptic plasticity in the central nervous system. Endogenous, plant-derived, synthetic cannabinoids bind to CB1R, initiating the inhibitory G-protein (Gi) and the β-arrestin ...
Haley K. Andersen   +5 more
doaj   +2 more sources

Chronic Fluoxetine Treatment Desensitizes Serotoninergic Inhibition of GABAergic Inputs and Intrinsic Excitability of Dorsal Raphe Serotonin Neurons [PDF]

open access: yesBrain Sciences
Background: Dorsal raphe serotonin (5-hydroxytryptamine, 5-HT) neurons are spontaneously active and release 5-HT that is critical for normal brain function and regulates mood and emotion.
Wei Zhang, Ying Jin, Fu-Ming Zhou
doaj   +2 more sources

Activation of GHSRs Facilitates the Excitability of Dentate Gyrus Granule Cells and Short-Term Spatial Memory via Multiple Ionic and Signaling Mechanisms. [PDF]

open access: yesAdv Biol (Weinh)
Ghrelin excites the dentate gyrus (DG) granule cells via GHSR‐mediated modulation of diverse ionic channels and activation of D1R, cAMP, and EPAC2. Similarly, overnight calorie restriction alters neuronal excitability in a ghrelin‐dependent manner. Infusion of ghrelin directly into the DG improves short‐term spatial memory in the Y‐maze, providing ...
Oraegbuna CS, Kola PK, Griggs SL, Lei S.
europepmc   +2 more sources

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