Results 1 to 10 of about 127,904 (323)

Selective activation of Gαob by an adenosine A₁ receptor agonist elicits analgesia without cardiorespiratory depression. [PDF]

Nat Commun, 2022
The development of therapeutic agonists for G protein-coupled receptors (GPCRs) is hampered by the propensity of GPCRs to couple to multiple intracellular signalling pathways.
Wall MJ, Hill E, Huckstepp R, Barkan K, Deganutti G, Leuenberger M, Preti B, Winfield I, Carvalho S, Suchankova A, Wei H, Safitri D, Huang X, Imlach W, La Mache C, Dean E, Hume C, Hayward S, Oliver J, Zhao FY, Spanswick D, Reynolds CA, Lochner M, Ladds G, Frenguelli BG.   +24 more
europepmc   +2 more sources

Adenosine stimulates the basolateral 50 pS K+ channel in renal proximal tubule via adenosine-A1 receptor [PDF]

Frontiers in Physiology, 2023
Background: The basolateral potassium channels play an important role in maintaining the membrane transport in the renal proximal tubules (PT) and adenosine receptors have been shown to regulate the trans-epithelial Na+ absorption in the PT.
Hao Liu, Qi Sun, Zheng Ding, Wensen Shi, Wen-Hui Wang, Chengbiao Zhang   +5 more
doaj   +2 more sources

The Signaling Pathways Involved in the Anticonvulsive Effects of the Adenosine A₁ Receptor. [PDF]

Int J Mol Sci, 2020
Adenosine acts as an endogenous anticonvulsant and seizure terminator in the brain. Many of its anticonvulsive effects are mediated through the activation of the adenosine A1 receptor, a G protein-coupled receptor with a wide array of targets. Activating
Spanoghe J, Larsen LE, Craey E, Manzella S, Van Dycke A, Boon P, Raedt R.   +6 more
europepmc   +2 more sources

Rolofylline, an adenosine A1−receptor antagonist, in acute heart failure [PDF]

New England Journal of Medicine, 2010
Background: Worsening renal function, which is associated with adverse outcomes, often develops in patients with acute heart failure. Experimental and clinical studies suggest that counterregulatory responses mediated by adenosine may be involved. We
Bloomfield, Daniel M, Cleland, John G F, Cotter, Gad, DeLucca, Paul, Dittrich, Howard C, Fu, Michael,, Givertz, Michael M, Mansoor, George A, Massie, Barry M, Metra, Marco, O'Connor, Christopher M, Ponikowski, Piotr, Salerno, Christina M, Teerlink, John R, Voors, Adriaan, Weatherley, Beth Davison   +15 more
core   +2 more sources

Adenosine A1 receptor activation mediates the developmental shift at layer 5 pyramidal cell synapses and is a determinant of mature synaptic strength [PDF]

Journal of Physiology, 2013
During the first postnatal month glutamatergic synapses between layer 5 pyramidal cells in the rodent neocortex switch from an immature state exhibiting high probability of neurotransmitter release, large unitary amplitude and synaptic depression to a ...
Dunwiddie TV, Magnus J. E. Richardson, Mark J. Wall, Michael I. Kerr   +3 more
core   +2 more sources

Cross-communication between Gi and Gs in a G-protein-coupled receptor heterotetramer guided by a receptor C-terminal domain [PDF]

BMC Biology, 2018
Background G-protein-coupled receptor (GPCR) heteromeric complexes have distinct properties from homomeric GPCRs, giving rise to new receptor functionalities.
Gemma Navarro, Arnau Cordomí, Marc Brugarolas, Estefanía Moreno, David Aguinaga, Laura Pérez-Benito, Sergi Ferre, Antoni Cortés, Vicent Casadó, Josefa Mallol, Enric I. Canela, Carme Lluís, Leonardo Pardo, Peter J. McCormick, Rafael Franco   +14 more
doaj   +4 more sources

Small molecule allosteric modulation of the adenosine A1 receptor [PDF]

Frontiers in Endocrinology, 2023
G protein-coupled receptors (GPCRs) represent the target for approximately a third of FDA-approved small molecule drugs. The adenosine A1 receptor (A1R), one of four adenosine GPCR subtypes, has important (patho)physiological roles in humans.
Anh T. N. Nguyen, Quan L. Tran, Jo-Anne Baltos, Samantha M. McNeill, Diep T. N. Nguyen, Lauren T. May   +5 more
doaj   +2 more sources

Adenosine Inhibits the Excitatory Synaptic Inputs to Basal Forebrain Cholinergic, GABAergic and Parvalbumin Neurons in mice [PDF]

Frontiers in Neurology, 2013
Coffee and tea contain the stimulants caffeine and theophylline. These compounds act as antagonists of adenosine receptors. Adenosine promotes sleep and its extracellular concentration rises in association with prolonged wakefulness, particularly in the ...
Chun eYang, Serena eFranciosi, Serena eFranciosi, Ritchie Edward Brown   +3 more
doaj   +3 more sources

Adenosine A1 receptor ligands bind to α-synuclein: implications for α-synuclein misfolding and α-synucleinopathy in Parkinson's disease. [PDF]

Transl Neurodegener, 2022
Jakova E, Moutaoufik MT, Lee JS, Babu M, Cayabyab FS.   +4 more
europepmc   +3 more sources

Long-term adenosine A1 receptor activation-induced sortilin expression promotes α-synuclein upregulation in dopaminergic neurons [PDF]

Neural Regeneration Research, 2020
Prolonged activation of adenosine A1 receptor likely leads to damage of dopaminergic neurons and subsequent development of neurodegenerative diseases.
Yun-Cheng Lv, An-Bo Gao, Jing Yang, Li-Yuan Zhong, Bo Jia, Shu-Hui Ouyang, Le Gui, Tian-Hong Peng, Sha Sun, Francisco S Cayabyab   +9 more
doaj   +2 more sources