Developments in the field of adenosine receptor (AR) agonists of the past years are presented
and discussed. Four different AR subtypes, A1, A2A, A2B, and A3, have been cloned from …

… Studies using these models have for the most part confirmed the known functions of A1
receptors … In summary, both agonists and antagonists for the A1 adenosine receptor have great …

… Potent adenosine receptor (AR) agonists and antagonists with high selectivity for the A 1
AR subtype have been developed during the past decades. However, some of the compounds …

… Table 1 Binding affinity of agonists at human A1, A2A and A3 adenosine receptor subtypes
(Ki-values in nM). For A2B receptors EC50-values (nM) for the agonist-mediated stimulation …

… the subtypes and is dictated in part by … agonists of A1 adenosine receptors has been
pursued by a number of groups in the effort to identify analogues that may produce less receptor …

… This article is part of a Special Issue entitled: “Adenosine Receptors”. … Several adenosine
receptor agonists and antagonists are currently evaluated in clinical trials. ► AR ligands are …

… Over a dozen of these selective agonists are now in clinical trials for various conditions, …
except for the endogenous AR agonist adenosine itself. A 1 AR agonists are in clinical trials for …

… A2A adenosine receptor agonists has been discontinued. Major problems include side effects
due to the wide distribution of adenosine receptors; low … part (Figure 1). Figure 2 shows the …

… agonist for rat A3 adenosine receptors (Fig. 2). IB-MECA 5 is 50-fold selective for A3 vs. …
of the A3 adenosine receptor subtype are, at least in part, elucidated. Series of selective …

… The neuroprotective effect of A 1 receptor activation is, in part, due to counteracting the …
adenosine receptor agonists [7,10,23,24]. The non-selective adenosine receptor agonist N 6 -2-(4…