Results 61 to 70 of about 2,269 (179)
The role of dimerisation in the cellular trafficking of G-protein-coupled receptors [PDF]
, 2010 The concept that G-protein-coupled receptors can exist as homomeric and/or heteromeric complexes is now well established. Despite this, how dynamic such interactions are and if this may be modulated during receptor trafficking remain topics of debate ...
Milligan, Graeme
core +1 more source
Threonine 180 Is Required for G-protein-coupled Receptor Kinase 3- and β-Arrestin 2-mediated Desensitization of the µ-Opioid Receptor in Xenopus Oocytes [PDF]
, 2001 To determine the sites in the µ-opioid receptor (MOR) critical for agonist-dependent desensitization, we constructed and coexpressed MORs lacking potential phosphorylation sites along with G-protein activated inwardly rectifying potassium channels ...
Celvert, Jeremy P. +4 more
core
RGS4 regulates partial agonism of the M2 muscarinic receptor-activated K+ currents. [PDF]
, 2014 Partial agonists are used clinically to avoid overstimulation of receptor-mediated signalling, as they produce a submaximal response even at 100% receptor occupancy.
Chen, I-Shan +3 more
core +2 more sources
Signal transduction pathway for the substance P‐induced inhibition of rat Kir3 (GIRK) channel [PDF]
The Journal of Physiology, 2005 Certain transmitters inhibit Kir3 (GIRK) channels, resulting in neuronal excitation. We analysed signalling mechanisms for substance P (SP)‐induced Kir3 inhibition in relation to the role of phosphatidylinositol 4,5‐bisphosphate (PIP2). SP rapidly – with a half‐time of ∼10 s with intracellular GTPγS and ∼14 s with intracellular GTP – inhibits a ...
Maki, Koike-Tani +7 more
openaire +2 more sources
British Journal of Pharmacology, EarlyView.Background and Purpose Adenosine is a potent regulator of neurotransmission and neuronal excitability, through activation of Gi coupled adenosine A1 receptors (A1Rs). Adenosine has gained interest as an anticonvulsant because of its endogenous involvement in ending seizure activity, but peripheral side effects require local application.
Erine Craey +8 more
wiley +1 more source
PLoS ONE, 2015 Endothelium lines the interior surface of vascular walls and regulates vascular tones. The endothelial cells sense and respond to chemical and mechanical stimuli in the circulation, and couple the stimulus signals to vascular smooth muscles, in which ...
Lihui Qu +11 more
doaj +1 more source
Ligand-induced closure of inward rectifier Kir6.2 channels traps spermine in the pore [PDF]
, 2003 Small organic amines block open voltage-gated K(+) channels and can be trapped by subsequent closure. Such studies provide strong evidence for voltage gating occurring at the intracellular end of the channel.
Nichols, Colin G, Phillips, L. Revell
core +3 more sources
Developmental regulation of G protein‐gated inwardly‐rectifying K+(GIRK/Kir3) channel subunits in the brain [PDF]
European Journal of Neuroscience, 2011 AbstractG protein‐gated inwardly‐rectifying K+(GIRK/family 3 of inwardly‐rectifying K+) channels are coupled to neurotransmitter action and can play important roles in modulating neuronal excitability. We investigated the temporal and spatial expression of GIRK1, GIRK2 and GIRK3 subunits in the developing and adult brain of mice and rats using ...
Fernández-Alacid, L +4 more
openaire +3 more sources
The Concise Guide to PHARMACOLOGY 2025/26: G protein‐coupled receptors
British Journal of Pharmacology, Volume 182, Issue S1, Page S24-S151, December 2025.The Concise Guide to Pharmacology 2025/26 marks the seventh edition in this series of biennial publications in the British Journal of Pharmacology. Presented in landscape format, the guide provides a comparative overview of the pharmacology of drug target families. The concise nature of the Concise Guide refers to the style of presentation, being clear,
Stephen P. H. Alexander +206 more
wiley +1 more source
Hydrogen sulfide inhibits Kir2 and Kir3 channels by decreasing sensitivity to the phospholipid phosphatidylinositol 4,5-bisphosphate (PIP2) [PDF]
Journal of Biological Chemistry, 2018 Inwardly rectifying potassium (Kir) channels establish and regulate the resting membrane potential of excitable cells in the heart, brain, and other peripheral tissues. Phosphatidylinositol 4,5-bisphosphate (PIP2) is a key direct activator of ion channels, including Kir channels.
Ha, J. +9 more
openaire +3 more sources