The Adenosine Receptors

1. Front Matter

   Pages i-xx

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2. Adenosine Receptors: The Status of the Art

   • Stefania Gessi, Stefania Merighi, Katia Varani

   Pages 1-11

3. Regulation of Extracellular Adenosine

   • Detlev Boison

   Pages 13-32

4. Adenosine Receptors: Structure, Distribution, and Signal Transduction

   • Stefania Merighi, Stefania Gessi, Pier Andrea Borea

   Pages 33-57

5. A1 Adenosine Receptor Agonists, Antagonists, and Allosteric Modulators

   • Zhan-Guo Gao, Dilip K. Tosh, Shanu Jain, Jinha Yu, Rama R. Suresh, Kenneth A. Jacobson

   Pages 59-89

6. A2A Adenosine Receptor: Structures, Modeling, and Medicinal Chemistry

   • Stefania Baraldi, Pier Giovanni Baraldi, Paola Oliva, Kiran S. Toti, Antonella Ciancetta, Kenneth A. Jacobson

   Pages 91-136

7. Medicinal Chemistry of A2B Adenosine Receptors

   • Christa E. Müller, Younis Baqi, Sonja Hinz, Vigneshwaran Namasivayam

   Pages 137-168

8. Medicinal Chemistry of the A3 Adenosine Receptor

   • Kenneth A. Jacobson, Dilip K. Tosh, Zhan-Guo Gao, Jinha Yu, Rama R. Suresh, Harsha Rao et al.

   Pages 169-198

9. Binding Thermodynamic Characteristics of Adenosine Receptor Ligands

   • Fabrizio Vincenzi, Katia Varani, Pier Andrea Borea

   Pages 199-215

10. Adenosine Receptors and Neuroinflammation

    • Antonella Ferrante, Roberta De Simone, Maria Antonietta Ajmone-Cat, Luisa Minghetti, Patrizia Popoli

    Pages 217-237

11. Adenosine Receptors as a Paradigm to Identify Dimer/Oligomers of G-Protein-Coupled Receptors and as Targets in Parkinson’s Disease and Schizophrenia

    • Gemma Navarro, Dasiel O. Borroto-Escuela, Kiell Fuxe, Rafael Franco

    Pages 239-258

12. Adenosine Receptors in Alzheimer’s Disease

    • Paula M. Canas, Rodrigo A. Cunha, Paula Agostinho

    Pages 259-280

13. What Is the Role of Adenosine Tone and Adenosine Receptors in Huntington’s Disease?

    • David Blum, En Chiang Chern, Maria Rosaria Domenici, Luc Buée, Ching Yeh Lin, Sergi Ferré et al.

    Pages 281-308

14. Role of Adenosine Receptors in Epileptic Seizures

    • Diogo Miguel Rombo, Joaquim Alexandre Ribeiro, Ana Maria Sebastião

    Pages 309-350

15. Adenosine and Oxygen/Glucose Deprivation in the Brain

    • Felicita Pedata, Ilaria Dettori, Lisa Gaviano, Elisabetta Coppi, Anna Maria Pugliese

    Pages 351-378

16. The Adenosine Receptor: A Homeostatic Neuromodulator for Fine-Tuning Control of Cognition

    • Jiang-Fan Chen

    Pages 379-411

17. The Adenosine-Receptor Axis in Chronic Pain

    • Daniela Salvemini, Timothy M. Doyle, Tally M. Largent-Milnes, Todd W. Vanderah

    Pages 413-437

18. Adenosine Signalling in the Injured Heart

    • Julia Hesse, Christina Alter, Jürgen Schrader

    Pages 439-460

19. Adenosine Receptors in the Lungs

    • Amir Pelleg, Riccardo Polosa

    Pages 461-470

20. Renal Adenosine in Health and Disease

    • H. Thomas Lee, Jurgen Schnermann

    Pages 471-498

This book traces the history of adenosine receptor research from molecular biology to medicinal chemistry to behavior, including their implications in disease and potential strategies as therapeutic targets. It provides the reader with a comprehensive overview of the adenosine receptors that includes information on all subtypes - A₁, A_2A, A_2B and A₃. Aspects addressed include the most up to date information on their functional distribution in the nervous and peripheral systems, behavioral roles in inflammation, cancer, pain and neurological diseases such as Huntington’s disease, Epilepsy, Parkinson’s disease and Alzheimer’s disease.

• molecular structure
• receptor subtypes
• research drug and development
• biological functions
• adenosine based pharmacotherapy
• diseases

• Department of Medical Sciences, University of Ferrara, Ferrara, Italy

  Pier Andrea Borea, Katia Varani, Stefania Gessi, Stefania Merighi, Fabrizio Vincenzi

Pier Andrea Borea received his degree in Chemistry Summa cum Laude from the University of Ferrara in 1967. He moved as Visiting Professor to Preclinical Research Department, Sandoz, Basel (CH) and to Medical Research Council Molecular Neurobiology Unit, Cambridge (UK). At present he is Honorary Professor of Pharmacology and member of the Board of Directors at the University of Ferrara. He is member of the Italian Society of Pharmacology and Purine Club. He has published 400 publications in international journals and contributed about 20 chapters to International Books. He has participated in more than 200 congresses, presenting main, oral and poster communications. He is also named as inventor in about 20 Patents. He has been invited to give about 50 Plenary Lectures at International Symposia and at several Universities. His main field of interest is represented by the study, at the molecular level, of drug-receptor interactions and in particular of the P1 adenosine receptor system.

Katia Varani received her degree in Biology in 1988 and her Ph.D. in Cellular and Molecular Pharmacology in 1995 from the University of Ferrara. She is currently Associate Professor of Pharmacology at the Medical Sciences Department of the University of Ferrara. Her research activity mainly involve pharmacological, biochemical and molecular characterization of adenosine receptors in human neurodegenerative diseases, chronic and neuropathic pain, inflammatory diseases and cancer.  She has published 250 publications on peer-reviewed international scientific journals, 15 book chapters and several communications in international and national congresses. She is member of the Italian Society of Pharmacology and Purine Club.

Stefania Gessi received her degree in Biology Summa cum Laude from University of Ferrara in 1994 and her Ph.D. in Cellular and Molecular Pharmacology in 2000 under the guidance of Professor Pier Andrea Borea. She moved at Centro RicercheSchering-Plough, Parco Scientifico San Raffaele (Milano) and at the Department of Physiology and Pharmacology, section of Molecular Neuropharmacology, Karolinska Institutet (Stockholm). She is currently Associate Professor of Pharmacology in the Medical Sciences Department of the University of Ferrara. Her research activity focused mainly on the pharmacological, biochemical and molecular study of adenosine receptors in inflammation and cancer and is documented by more than 130 publications on peer-reviewed international scientific journals, 18 book chapters and several communications in international and national congresses. She is member of the Italian Society of Pharmacology and Purine Club.

Stefania Merighi received her degree in Biology Summa cum Laude at the University of Ferrara (Italy) in 1997 and obtained her Ph.D. in Cellular and Molecular Pharmacology at the same University in 2003. Currently, she is Associate Professor of Pharmacology at the University of Ferrara, a position she has held since 2017. Her research activities primarily focus on the pharmacological, biochemical and molecular study of GPCRs in oncology and neuroinflammation and has published extensively in this area. Her research activity is documented by more than 100 publications on peer-reviewed International scientific journals and several communications in International and National congresses. She is member of the Italian Society of Pharmacology and Purine Club.

Fabrizio Vincenzi received his degree in Biology from University of Ferrara in 2004 and obtained his Ph.D. in Cellular and Molecular Pharmacology in 2008 at the section of Pharmacology of the University of Ferrara. His main research field is represented by the study of the drug-receptor interaction with specific interest in the thermodynamic and kinetic aspect of the ligand-receptor binding. He primarily focused his research on the study of G-protein coupled receptors and in particular on adenosine receptors and their involvement in neurodegenerative diseases, pain, chronic inflammatory diseases, anxiety and cancer. He has published 80 scientific papers in peer-reviewed international journals and is member of the Italian Society of Pharmacology and Purine Club.

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