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A3 Adenosine Receptor Antagonists: History and Future Perspectives

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A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Abstract

The potential employment of selective A3 adenosine receptor (A3AR) antagonists in the therapeutic treatment of important pathologies, such as asthma, inflammation, neurodegeneration, glaucoma and cancer, is subject to intensive studies because of the considerable role of this receptor in a number of pathophysiological processes. A wide number of compounds exerting high potency and selectivity in antagonizing the hA3 AR has been so far recognized being generally characterized by a remarkable structural diversity: nitrogen-containing aromatic monocyclic (thiazoles, thiadiazoles, 1,4-dihydropyridines, pyridines, 2-mercaptopyrimidines), bicyclic (flavonoid, isoquinoline, quinozalines, (aza)adenines), tricyclic systems (pyrazoloquinolines, triazoloquinoxalines, pyrazolotriazolopyrimidines, triazolopurines, tricyclic xanthines). The latest identification of nucleoside-derived antagonists, structurally related to the endogenous ligand, opened new frontiers for the elucidation of the therapeutic potential of this kind of ligands. Probably as a result of the enigmatic physiological role of A3AR, whose activation seems related to opposite effects concerning tissues protection in inflammatory and cancer cells, a few molecules have till now reached the preclinical investigation phase.

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Authors and Affiliations

  1. Dipartimento di Scienze Farmaceutiche, Università di Ferrara, 44100, Ferrara, Italy

    Pier Giovanni Baraldi

  2. Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100, Ferrara, Italy

    Pier Giovanni Baraldi, Romeo Romagnoli, Giulia Saponaro, Stefania Baraldi, Mojgan Aghazadeh Tabrizi & Delia Preti

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  1. Pier Giovanni Baraldi
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  2. Romeo Romagnoli
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  3. Giulia Saponaro
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  4. Stefania Baraldi
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  5. Mojgan Aghazadeh Tabrizi
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  6. Delia Preti
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Correspondence to Pier Giovanni Baraldi .

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  1. Ist. Farmacologia, Universita Ferrara, Via Fossato di Mortara 64 B, Ferrara, 44100, Italy

    Pier Andrea Borea

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Baraldi, P.G., Romagnoli, R., Saponaro, G., Baraldi, S., Tabrizi, M.A., Preti, D. (2010). A3 Adenosine Receptor Antagonists: History and Future Perspectives. In: Borea, P. (eds) A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics. Springer, Dordrecht. https://doi.org/10.1007/978-90-481-3144-0_7

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