Therapeutic Potential of Highly Selective A<sub>3</sub> Adenosine Receptor Ligands in the Central and Peripheral Nervous System

Elisabetta Coppi; Federica Cherchi; Martina Venturini; Elena Lucarini; Renato Corradetti; Lorenzo Di Cesare Mannelli; Carla Ghelardini; Felicita Pedata; Anna Maria Pugliese

doi:10.3390/molecules27061890

Molecules (Mar 2022)

Therapeutic Potential of Highly Selective A<sub>3</sub> Adenosine Receptor Ligands in the Central and Peripheral Nervous System

Elisabetta Coppi,
Federica Cherchi,
Martina Venturini,
Elena Lucarini,
Renato Corradetti,
Lorenzo Di Cesare Mannelli,
Carla Ghelardini,
Felicita Pedata,
Anna Maria Pugliese

Affiliations

Elisabetta Coppi: Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Division of Pharmacology and Toxicology, University of Florence, 50139 Florence, Italy
Federica Cherchi: Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Division of Pharmacology and Toxicology, University of Florence, 50139 Florence, Italy
Martina Venturini: Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Division of Pharmacology and Toxicology, University of Florence, 50139 Florence, Italy
Elena Lucarini: Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Division of Pharmacology and Toxicology, University of Florence, 50139 Florence, Italy
Renato Corradetti: Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Division of Pharmacology and Toxicology, University of Florence, 50139 Florence, Italy
Lorenzo Di Cesare Mannelli: Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Division of Pharmacology and Toxicology, University of Florence, 50139 Florence, Italy
Carla Ghelardini: Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Division of Pharmacology and Toxicology, University of Florence, 50139 Florence, Italy
Felicita Pedata: Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Division of Pharmacology and Toxicology, University of Florence, 50139 Florence, Italy
Anna Maria Pugliese: Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Division of Pharmacology and Toxicology, University of Florence, 50139 Florence, Italy

DOI: https://doi.org/10.3390/molecules27061890
Journal volume & issue: Vol. 27, no. 6
p. 1890

Abstract

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Ligands of the Gi protein-coupled adenosine A3 receptor (A3R) are receiving increasing interest as attractive therapeutic tools for the treatment of a number of pathological conditions of the central and peripheral nervous systems (CNS and PNS, respectively). Their safe pharmacological profiles emerging from clinical trials on different pathologies (e.g., rheumatoid arthritis, psoriasis and fatty liver diseases) confer a realistic translational potential to these compounds, thus encouraging the investigation of highly selective agonists and antagonists of A3R. The present review summarizes information on the effect of latest-generation A3R ligands, not yet available in commerce, obtained by using different in vitro and in vivo models of various PNS- or CNS-related disorders. This review places particular focus on brain ischemia insults and colitis, where the prototypical A3R agonist, Cl-IB-MECA, and antagonist, MRS1523, have been used in research studies as reference compounds to explore the effects of latest-generation ligands on this receptor. The advantages and weaknesses of these compounds in terms of therapeutic potential are discussed.

Published in Molecules

ISSN: 1420-3049 (Online)
Publisher: MDPI AG
Country of publisher: Switzerland
LCC subjects: Science: Chemistry: Organic chemistry
Website: http://www.mdpi.com/journal/molecules

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Abstract

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