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Ligands for Adenosine receptors (ARs or alternately P1 receptors)

Adenosine receptors belong to the G protein-coupled receptor (GPCR) superfamily. Consisting of four subclasses (A1, A2A, A2B and A3), they sense a particularly diverse set of ligands and have been linked to various clinical indications such as cancer, diabetes, cardiovascular, inflammatory and neural diseases, as well as immunogenic disorders. To address ligand interactions and functions of adenosine receptors and to facilitate the search for potential therapeutics we offer broad selection of well-established agonists and antagonists, namely adenosine-derived nucleosides, nucleotides and heterocycles.

Please click the receptor subclass of interest for appropriate adenosine receptor ligands.


Selected References

Jacobson (2013) Structure based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates. J. Med. Chem. 56:3749.
Shenone et al. (2010) A1 Receptors Ligands: Past, present and future trends. Cur. Topics in Medicin. Chem. 10:878.
Volonte et al. (2009) Membrane components and purinergic signalling: the purinome, a complex interplay among ligands, degrading enzymes, receptors and transporters. FEBS J. 276:318.
Yegutkin (2008) Nucleotide and nucleoside converting enzymes: Important modulators of purinergic signalling cascade. Biochim. Biophys. Acta 1783:673.
Ishiwata et al. (2007) PET tracers for mapping adenosine receptors as probes for diagnosis of CNS disorders. Central Nervous System Agents in Medicinal Chemistry 7:57.
Wong et al. (2006) Endogenous activation of adenosine A1 receptors, but not P2X receptors, during high frequency synaptic transmission at the calyx of Held. J. Neurophysiology 95 (6):3336.
Masino et al. (2002) Modulation of hippocampal glutamatergic transmission by ATP is dependent on adenosine A1 receptors. J. Pharmacol. and Experiment. Therapeutics 303 (1):356.