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Chemical Probes for the Adenosine Receptors

Department of Chemical and Pharmaceutical Sciences, University of Trieste, Via Licio Giorgeri 1, 34127 Trieste, Italy
Author to whom correspondence should be addressed.
Pharmaceuticals 2019, 12(4), 168;
Received: 26 September 2019 / Revised: 4 November 2019 / Accepted: 7 November 2019 / Published: 12 November 2019
(This article belongs to the Special Issue Adenosine Receptors as Attractive Targets in Human Diseases)
Research on the adenosine receptors has been supported by the continuous discovery of new chemical probes characterized by more and more affinity and selectivity for the single adenosine receptor subtypes (A1, A2A, A2B and A3 adenosine receptors). Furthermore, the development of new techniques for the detection of G protein-coupled receptors (GPCR) requires new specific probes. In fact, if in the past radioligands were the most important GPCR probes for detection, compound screening and diagnostic purposes, nowadays, increasing importance is given to fluorescent and covalent ligands. In fact, advances in techniques such as fluorescence resonance energy transfer (FRET) and fluorescent polarization, as well as new applications in flow cytometry and different fluorescence-based microscopic techniques, are at the origin of the extensive research of new fluorescent ligands for these receptors. The resurgence of covalent ligands is due in part to a change in the common thinking in the medicinal chemistry community that a covalent drug is necessarily more toxic than a reversible one, and in part to the useful application of covalent ligands in GPCR structural biology. In this review, an updated collection of available chemical probes targeting adenosine receptors is reported. View Full-Text
Keywords: adenosine receptors; fluorescent ligands; radioligands; radiotracers; covalent ligands; GPCR probes adenosine receptors; fluorescent ligands; radioligands; radiotracers; covalent ligands; GPCR probes
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Federico, S.; Lassiani, L.; Spalluto, G. Chemical Probes for the Adenosine Receptors. Pharmaceuticals 2019, 12, 168.

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