Results 1 to 10 of about 124,204 (359)

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

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

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

AMP Is an Adenosine A1 Receptor Agonist* [PDF]

Journal of Biological Chemistry, 2012
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, Ilia Korboukh, E. Hull-Ryde, Jian Jin, W. Janzen, S. Frye, M. Zylka   +6 more
semanticscholar   +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

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

Positive allosteric mechanisms of adenosine A₁ receptor-mediated analgesia. [PDF]

Nature, 2021
Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, White PJ, Scammells P, May LT, Sexton PM, Danev R, Miao Y, Glukhova A, Imlach WL, Christopoulos A.   +23 more
europepmc   +2 more sources

Adenosine A1 Receptor Agonist 2-chloro-N6-cyclopentyladenosine and Hippocampal Excitability During Brain Development in Rats [PDF]

Frontiers in Pharmacology, 2019
Objective: The adenosinergic system may influence excitability in the brain. Endogenous and exogenous adenosine has anticonvulsant activity presumably by activating A1 receptors.
Petr Fabera, Petr Fabera, Martina Parizkova, Martina Parizkova, Libor Uttl, Libor Uttl, Katerina Vondrakova, Katerina Vondrakova, Hana Kubova, Grygoriy Tsenov, Grygoriy Tsenov, Pavel Mares   +11 more
doaj   +2 more sources

Anti-inflammatory preconditioning by agonists of adenosine A1 receptor. [PDF]

PLoS ONE, 2008
BackgroundAdenosine levels rise during inflammation and modulate inflammatory responses by engaging with four different G protein-coupled receptors. It is suggested that adenosine exhibits pro-inflammatory effects through its A(1) receptor (A(1)R), and ...
Sigal Nakav, Cidio Chaimovitz, Yuval Sufaro, Eli C Lewis, Gad Shaked, David Czeiger, Moshe Zlotnik, Amos Douvdevani   +7 more
doaj   +4 more sources