Interplay between metabotropic glutamate type 4 and adenosine type 1 receptors modulate synaptic transmission in the cerebellar cortex [PDF]
The synapses between parallel fibers and Purkinje cells play a pivotal role in cerebellar function. They are intricately governed by a variety of presynaptic receptors, notably by type 4 metabotropic glutamate (mGlu4) receptors and type 1 adenosine (A1 ...
Simon Bossi+2 more
doaj +6 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]
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+3 more
core +2 more sources
AMP Is an Adenosine A1 Receptor Agonist* [PDF]
Background: There is no known receptor for the nucleotide AMP. Results: AMP directly activates the adenosine A1 receptor (A1R) but not the adenosine A2B receptor. Conclusion: A1R is a receptor for adenosine and AMP.
Joseph E. Rittiner+6 more
semanticscholar +4 more sources
Allosteric interactions at adenosine A1 and A3 receptors: new insights into the role of small molecules and receptor dimerization [PDF]
Keywords:adenosine;allosterism;receptor;GPCR;dimerization;biased signalling The purine nucleoside adenosine is present in all cells in tightly regulated concentrations. It is released under a variety of physiological and pathophysiological conditions to
Albrecht-Kupper+114 more
core +3 more sources
This study was undertaken in order to investigate the effect of chronic treatment with 5′-chloro-5′-deoxy-(±)-ENBA, a potent and highly selective agonist of human adenosine A1 receptor, on thermal hyperalgesia and mechanical ...
Livio Luongo+10 more
doaj +2 more sources
Cross-communication between Gi and Gs in a G-protein-coupled receptor heterotetramer guided by a receptor C-terminal domain [PDF]
Background G-protein-coupled receptor (GPCR) heteromeric complexes have distinct properties from homomeric GPCRs, giving rise to new receptor functionalities.
Gemma Navarro+14 more
doaj +4 more sources
Adenosine A1 receptor antagonists in clinical research and development. [PDF]
Selective adenosine A1 receptor antagonists targeting renal microcirculation are novel pharmacologic agents that are currently under development for the treatment of acute heart failure as well as for chronic heart failure. Despite several studies showing improvement of renal function and/or increased diuresis with adenosine A1 antagonists ...
B. Hocher
semanticscholar +4 more sources
Rolofylline, an adenosine A1−receptor antagonist, in acute heart failure [PDF]
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.+14 more
core +2 more sources
Target screening and optimization of candidate compounds for breast cancer treatment using bioinformatics and computational chemistry approaches [PDF]
ObjectivesThis study aimed to identify critical therapeutic targets and design potent antitumor compounds for breast cancer treatment through an integrated bioinformatics and computational chemistry approach.MethodsWe conducted initial screening and ...
Jian Xu, Xue Li, Yiduo Jia, Yiduo Jia
doaj +2 more sources
Frequency Facilitation at Mossy Fiber–CA3 Synapses of Freely Behaving Rats Contributes to the Induction of Persistent LTD via an Adenosine-A1 Receptor-Regulated Mechanism [PDF]
Frequency facilitation (FF), comprising a rapid and multiple-fold increase in the magnitude of evoked field potentials, is elicited by low-frequency stimulation (LFS) at mossy fiber–CA3 synapses.
Abbracchio+53 more
core +3 more sources