A Series of Ligands Displaying a Remarkable Agonistic−Antagonistic Profile at the Adenosine A1 Receptor

LCW Chang… - Journal of medicinal …, 2005 - ACS Publications
Adenosine receptor agonists are usually variations of the natural ligand, adenosine. The
ribose moiety in the ligand has previously been shown to be of great importance for the …

Site-directed Mutagenesis Identifies Residues Involved in Ligand Recognition in the Human A2a Adenosine Receptor∗

J Kim, J Wess, AM van Rhee, T Schöneberg… - Journal of Biological …, 1995 - ASBMB
The A 2a adenosine receptor is a member of the G-protein coupled receptor family, and its
activation stimulates cyclic AMP production. To determine the residues which are involved in …

New strategies for the synthesis of A3 adenosine receptor antagonists

PG Baraldi, A Bovero, F Fruttarolo, R Romagnoli… - Bioorganic & medicinal …, 2003 - Elsevier
New A3 adenosine receptor antagonists were synthesized and tested at human adenosine
receptor subtypes. An advanced synthetic strategy permitted us to obtain a large amount of …

The role of receptor structure in determining adenosine receptor activity

ME Olah, GL Stiles - Pharmacology & therapeutics, 2000 - Elsevier
Adenosine produces a wide variety of physiological effects through the activation of cell
surface adenosine receptors (ARs). ARs are members of the G-protein-coupled receptor …

Cloned receptors and cardiovascular responses to adenosine.

AL Tucker, J Linden - Cardiovascular research, 1993 - europepmc.org
Four subtypes of adenosine receptors have recently been cloned from thyroid, brain and
testis. In this review we have summarised properties of these purinergic receptors. The …

Emerging adenosine receptor agonists

ZG Gao, KA Jacobson - Expert opinion on emerging drugs, 2007 - Taylor & Francis
Adenosine receptors (ARs) are a four-member subfamily of G protein-coupled receptors and
are major targets of caffeine and theophylline. There are four subtypes of ARs, designated …

[HTML][HTML] Cloning, expression, and characterization of the unique bovine A1 adenosine receptor. Studies on the ligand binding site by site-directed mutagenesis.

ME Olah, H Ren, J Ostrowski, KA Jacobson… - Journal of Biological …, 1992 - Elsevier
The bovine brain A1 adenosine receptor (A1AR) is distinct from other A1ARs in that it
displays the unique agonist potency series of N6-R-phenylisopropyladenosine (R-PIA) …

Adenosine receptors and cancer

P Fishman, S Bar-Yehuda, M Synowitz… - Adenosine Receptors in …, 2009 - Springer
Abstract The A 1, A 2A, A 2B and A 3 G-protein-coupled cell surface adenosine receptors
(ARs) are found to be upregulated in various tumor cells. Activation of the receptors by …

Antagonists of the Human A2A Adenosine Receptor. 4. Design, Synthesis, and Preclinical Evaluation of 7-Aryltriazolo[4,5-d]pyrimidines

RJ Gillespie, SJ Bamford, R Botting… - Journal of medicinal …, 2009 - ACS Publications
Antagonism of the human A2A receptor has been implicated as a point of therapeutic
intervention in the alleviation of the symptoms associated with Parkinson's disease. This is …

[HTML][HTML] Molecular modeling of adenosine receptors. I. The ligand binding site on the A1 receptor

AP Ijzerman, PJM van Galen… - Drug design and …, 1992 - ncbi.nlm.nih.gov
The amino acid sequence of the canine adenosine A 1 receptor and the atomic coordinates
of a structurally related protein, bacteriorhodopsin, were combined to generate a three …