Adenosine receptors as drug targets—what are the challenges?

JF Chen, HK Eltzschig, BB Fredholm - Nature reviews Drug discovery, 2013 - nature.com
Adenosine signalling has long been a target for drug development, with adenosine itself or
its derivatives being used clinically since the 1940s. In addition, methylxanthines such as …

Medicinal chemistry of adenosine, P2Y and P2X receptors

KA Jacobson, CE Müller - Neuropharmacology, 2016 - Elsevier
Pharmacological tool compounds are now available to define action at the adenosine (ARs),
P2Y and P2X receptors. We present a selection of the most commonly used agents to study …

Historical and current adenosine receptor agonists in preclinical and clinical development

KA Jacobson, DK Tosh, S Jain, ZG Gao - Frontiers in cellular …, 2019 - frontiersin.org
Adenosine receptors (ARs) function in the body's response to conditions of pathology and
stress associated with a functional imbalance, such as in the supply and demand of …

Focusing on adenosine receptors as a potential targeted therapy in human diseases

WI Effendi, T Nagano, K Kobayashi, Y Nishimura - Cells, 2020 - mdpi.com
Adenosine is involved in a range of physiological and pathological effects through
membrane-bound receptors linked to G proteins. There are four subtypes of adenosine …

[HTML][HTML] Recent developments in adenosine receptor ligands and their potential as novel drugs

CE Müller, KA Jacobson - Biochimica et Biophysica Acta (BBA) …, 2011 - Elsevier
Medicinal chemical approaches have been applied to all four of the adenosine receptor
(AR) subtypes (A1, A2A, A2B, and A3) to create selective agonists and antagonists for each …

Adenosine A2A Receptor as a Drug Discovery Target

M de Lera Ruiz, YH Lim, J Zheng - Journal of medicinal chemistry, 2014 - ACS Publications
The adenosine A2A receptor is a G-protein-coupled receptor (GPCR) that has been
extensively studied during the past few decades because it offers numerous possibilities for …

Cardiac purinergic signalling in health and disease

G Burnstock, A Pelleg - Purinergic signalling, 2015 - Springer
This review is a historical account about purinergic signalling in the heart, for readers to see
how ideas and understanding have changed as new experimental results were published …

Mechanisms by which adenosine restores conduction in dormant canine pulmonary veins

T Datino, L Macle, XY Qi, A Maguy, P Comtois… - Circulation, 2010 - Am Heart Assoc
Background—Adenosine acutely reconnects pulmonary veins (PVs) after radiofrequency
application, revealing “dormant conduction” and identifying PVs at risk of reconnection, but …

Metabolic autocrine regulation of neurons involves cooperation among pannexin hemichannels, adenosine receptors, and KATP channels

M Kawamura, DN Ruskin, SA Masino - Journal of neuroscience, 2010 - Soc Neuroscience
Metabolic perturbations that decrease or limit blood glucose—such as fasting or adhering to
a ketogenic diet—reduce epileptic seizures significantly. To date, the critical links between …

Treatment of chronic neuropathic pain: purine receptor modulation

KA Jacobson, LA Giancotti, F Lauro, F Mufti… - Pain, 2020 - journals.lww.com
Extracellular nucleosides and nucleotides have widespread functions in responding to
physiological stress. The “purinome” encompasses 4 G-protein-coupled receptors (GPCRs) …