Results 1 to 10 of about 68,176 (222)

Deciphering the Agonist Binding Mechanism to the Adenosine A1 Receptor. [PDF]

ACS Pharmacol Transl Sci, 2021
ABSTRACTDespite being amongst the most characterized G protein-coupled receptors (GPCRs), adenosine receptors (ARs) have always been a difficult target in drug design. To date, no agonist other than the natural effector and the diagnostic regadenoson has been approved for human use.
Deganutti G, Barkan K, Preti B, Leuenberger M, Wall M, Frenguelli BG, Lochner M, Ladds G, Reynolds CA.   +8 more
europepmc   +9 more sources

Multisite Model of Allosterism for the Adenosine A1 Receptor [PDF]

Journal of Chemical Information and Modeling, 2020
ABSTRACTDespite being a target for about one-third of approved drugs, G protein-coupled receptors (GPCRs) still represent a tremendous reservoir for therapeutic strategies against countless diseases. For example, several cardiovascular and central nervous systems conditions could benefit from clinical agents that activate the adenosine 1 receptor (A1R),
Giuseppe Deganutti, Kerry Barkan, Graham Ladds, Christopher A Reynolds   +3 more
openaire   +3 more sources

Adenosine receptors in GtoPdb v.2021.2 [PDF]

, 2021
Adenosine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Adenosine Receptors [110]) are activated by the endogenous ligand adenosine (potentially inosine also at A3 receptors).
Fredholm, Bertil B., Frenguelli, Bruno G., Hills, Rebecca, IJzerman, Adriaan P., Jacobson, Kenneth A., Klotz, Karl-Norbert, Linden, Joel, Müller, Christa E., Schwabe, Ulrich, Stiles, Gary L.   +9 more
core   +2 more sources

Immunolocalization of A1 Adenosine Receptors in Mammalian Spermatozoa [PDF]

Journal of Histochemistry & Cytochemistry, 2000
The presence of A1 adenosine receptors (A1AR) in mammalian spermatozoa was previously demonstrated by radiochemical and immunochemical detection. This study was performed to investigate the cellular location of the A1AR to determine whether these receptors were somehow connected with ecto-adenosine deaminase and to evaluate their function in calcium ...
MINELLI, Alba, ALLEGRUCCI, Cinzia, Piomboni P., MANNUCCI, Roberta, Lluis C., Franco R.   +5 more
openaire   +5 more sources

Adenosine receptors in GtoPdb v.2023.1 [PDF]

, 2023
Adenosine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Adenosine Receptors [112]) are activated by the endogenous ligand adenosine (potentially inosine also at A3 receptors).
Fredholm, Bertil B., Frenguelli, Bruno G., Hills, Rebecca, IJzerman, Adriaan P., Jacobson, Kenneth A., Klotz, Karl-Norbert, Linden, Joel, Müller, Christa E., Schwabe, Ulrich, Stiles, Gary L.   +9 more
core   +2 more sources

AMP Is an Adenosine A1 Receptor Agonist [PDF]

Journal of Biological Chemistry, 2012
Numerous receptors for ATP, ADP, and adenosine exist; however, it is currently unknown whether a receptor for the related nucleotide adenosine 5′-monophosphate (AMP) exists. Using a novel cell-based assay to visualize adenosine receptor activation in real time, we found that AMP and a non-hydrolyzable AMP analog (deoxyadenosine 5′-monophosphonate, ACP)
Joseph E. Rittiner, Emily A. Hull-Ryde, Mark J. Zylka, William P. Janzen, Stephen V. Frye, Jian Jin, Ilia Korboukh   +6 more
openaire   +3 more sources

Photoaffinity labeling of A1-adenosine receptors. [PDF]

Journal of Biological Chemistry, 1985
The ligand-binding subunit of the A1-adenosine receptor has been identified by photoaffinity labeling. A photolabile derivative of R-N6-phenylisopropyladenosine, R-2-azido-N6-p-hydroxyphenylisopropyladenosine (R-AHPIA), has been synthesized as a covalent specific ligand for A1-adenosine receptors.
Klotz, Karl-Norbert, Cristalli, G., Grifantini, M., Vittori, S., Lohse, M. J.   +4 more
openaire   +3 more sources

Stimulation of endothelial adenosine Al receptors enhances adhesion of neutrophils in the intact guinea pig coronary system [PDF]

, 1994
Objective: The primary aim was to determine the action of pathophysiologically relevant adenosine concentrations (0.1-1 μM) on adhesion of neutrophils to coronary endothelium.
Becker, Bernhard F., Gerlach, E., Raschke, P., Zahler, Stefan   +3 more
core   +1 more source

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

, 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   +1 more source

Selective reduction of neurotransmitter release by cAMP-dependent pathways in mouse detrusor [PDF]

, 2022
Parasympathetic nerve-mediated contractions of detrusor smooth muscle are generated by ATP and acetylcholine (ACh) release from efferent nerve terminals. In humans, ACh is responsible for detrusor contractions in normal human bladders, whereas ATP has an
Chakrabarty, Basu, Drake, Marcus J, Fry, Christopher H, Kanai, Anthony J   +3 more
core   +3 more sources