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Cited by 783Adenosine and Purinergic SignalingBiochemical and Molecular ResearchPain Mechanisms and Treatments

Pharmacology of Adenosine Receptors: The State of the Art

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Borea, Pier Andrea, Gessi, Stefania, Merighi, Stefania, Vincenzi, Fabrizio, Varani, Katia·2018·Physiological Reviews
DOI 10.1152/physrev.00049.2017
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Abstract

Adenosine is a ubiquitous endogenous autacoid whose effects are triggered through the enrollment of four G protein-coupled receptors: A 1, A 2A, A 2B, and A 3. Due to the rapid generation of adenosine from cellular metabolism, and the widespread distribution of its receptor subtypes in almost all organs and tissues, this nucleoside induces a multitude of physiopathological effects, regulating central nervous, cardiovascular, peripheral, and immune systems. It is becoming clear that the expression patterns of adenosine receptors vary among cell types, lending weight to the idea that they may be both markers of pathologies and useful targets for novel drugs. This review offers an overview of current knowledge on adenosine receptors, including their characteristic structural features, molecular interactions and cellular functions, as well as their essential roles in pain, cancer, and neurodegenerative, inflammatory, and autoimmune diseases. Finally, we highlight the latest findings on molecules capable of targeting adenosine receptors and report which stage of drug development they have reached.

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  • Post-marketing surveillance and pharmacovigilance data have not revealed any significant safety concerns for either PDRN or PN.

    “Furthermore, post-marketing surveillance and pharmacovigilance data have not revealed any significant safety concerns for either compound [19,151].”

    From Comparison of Polynucleotide and Polydeoxyribonucleotide in Dermatology: Molecular Mechanisms and Clinical Perspectives (2025) · cites this paper as [151]

    The A2A AR section discusses PDRN’s efficacy in a diabetic-foot-ulcer trial, but does not address its post-marketing safety. Searches for pharmacovigilance, post-marketing surveillance, and PDRN or PN adverse events found no passage supporting the claim about either compound. (LLM, conf=0.74)

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Cited by

Sorted by citations

Authors
Borea, P. A., Gessi, S., Merighi, S., Vincenzi, F., & Varani, K.
Affiliations
University of Ferrara (IT)
ORCID
Venue
Physiological Reviews
Publisher
American Physiological Society
Published
2018-07-01
Volume
98
Issue
3
Pages
1591-1625
ISSN
  • 0031-9333 (ISSN-L)
  • 1522-1210
DOI
10.1152/physrev.00049.2017
OpenAlex
W2805539079
Cited by
783
References
8
Citations by year
2026: 79 · 2025: 86 · 2024: 120 · 2023: 107 · 2022: 133 · 2021: 117 · 2020: 80 · 2019: 56 · 2018: 4
FWCI
7.72
Type
journal article
Language
en
Open access
Locations
  • Physiological Reviews (publishedVersion)
  • PubMed (publishedVersion)
  • Institutional Research Information System University of Ferrara (University of Ferrara) (submittedVersion, other-oa)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Physiology › Adenosine and Purinergic Signaling
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Biochemical and Molecular Research
  • Health Sciences › Medicine › Physiology › Pain Mechanisms and Treatments
Keywords
adenosine receptors, adenosine receptor subtypes, receptor structure, receptor signaling, adenosine, pain, cancer, neurodegenerative diseases, inflammatory diseases, autoimmune disease, adenosine receptor agonists, adenosine receptor antagonists, drug development, therapeutic target
MeSH terms
Adenosine, Animals, Autoimmune Diseases, Cardiovascular Diseases, Humans, Neoplasms, Nervous System Diseases, Molecular Structure, Signal Transduction, Receptors, Purinergic P1, Purinergic P1 Receptor Agonists, Purinergic P1 Receptor Antagonists

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