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A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Editors: Borea, Pier Andrea

DOI: 10.1007/978-90-481-3144-0

ISBN: 978-90-481-3143-3

Publisher: Springer Netherlands - Springer Journals

Nov 6, 2009

1 - 10 of 16 Chapters

Available

From Hypertension (+) to Asthma: Interactions with the Adenosine A3 Receptor from a Personal Perspective

Fozard, John R.

Pages: 3 –26

[I present in this chapter an account of my own personal ‘interaction’ with the adenosine A3 receptor. This started before the A3 receptor was discovered as an offshoot of an interest in adenosine A1 receptor agonists as a novel approach to the treatment of hypertension and emerged almost a...
Available

Thermodynamic Analysis in Drug–Receptor Binding: The A3 Adenosine Receptor

Borea, Pier Andrea; Gessi, Stefania; Merighi, Stefania; Varani, Katia

Pages: 29 –48

[Receptor binding thermodynamics is a powerful tool to gain deep insight, at the molecular level, of the events which occur during drug–receptor interactions. This paper deals with the study of the A3 adenosine receptors in the general scenario of all receptors studied so far from this point of...
Available

Pharmacology and Molecular Biology of A3 Adenosine Receptors

Klotz, Karl-Norbert

Pages: 49 –58

[Adenosine is an important metabolite and a building block for many biologically relevant molecules. Most abundantly, it contributes the purine base adenine and a ribose to ATP which as an energy-providing compound occurs in millimolar concentrations in every cell. Such high concentrations of ATP...
Available

Regulation of Second Messenger Systems and Intracellular Pathways

Merighi, Stefania; Simioni, Carolina; Lane, Rob; Ijzerman, Adriaan P.

Pages: 61 –73

[The A3 adenosine receptor is a G protein-coupled receptor linked to classical second messenger pathways such as those for cAMP production and phospholipase C. In addition, the receptor couples to mitogen-activated protein kinases (MAPK) and to the phosphatidylinositol 3-kinase/protein kinase B...
Available

The Desensitisation as A3 Adenosine Receptor Regulation: Physiopathological Implications

Trincavelli, Maria Letizia; Ciampi, Osele; Martini, Claudia

Pages: 75 –90

[A3 adenosine receptors are subjected to fast desensitisation, internalisation and down regulation after agonist exposure. As almost all G-protein coupled receptors, these regulatory mechanisms are mediated by receptor phosphorylation in a process that results in the recruitment of arrestins....
Available

A3 Adenosine Receptor Agonists: History and Future Perspectives

Jacobson, Kenneth A.; Gao, Zhan-Guo; Tosh, Dilip K.; Sanjayan, Gangadhar J.; de Castro, Sonia

Pages: 93 –120

[IB-MECA, the first selective A3 adenosine receptor (A3AR) agonist, was reported in 1993, and since then numerous adenosine derivatives have been modified to optimize their interaction with the A3AR. IB-MECA (CF101) and its 2-chloro analogue, Cl-IB-MECA (CF102) are in Phase II clinical trials for...
Available

A3 Adenosine Receptor Antagonists: History and Future Perspectives

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

Pages: 121 –147

[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...
Available

Molecular Modeling and Reengineering of A3 Adenosine Receptors

Moro, Stefano; Morizzo, Erika; Jacobson, Kenneth A.

Pages: 149 –161

[The development of ligands for the A3 adenosine receptor (AR) has been directed mainly by traditional medicinal chemistry, but the influence of structure-based approaches is increasing. Rhodopsin-based homology modeling had been used for many years to obtain three-dimensional models of the A3AR,...
Available

Adenosine A3 Receptor Signaling in the Central Nervous System

Pedata, Felicita; Pugliese, Anna Maria; Sebastião, Ana M.; Ribeiro, Joaquim A.

Pages: 165 –188

[Adenosine A3 receptors are widely distributed in the central nervous system but are expressed at a low level and have lower affinity for adenosine in comparison to the A1 and A2A receptors. Nevertheless, they appear to tonically modulate motor activity as pointed out in A3 receptor-deleted mice.]
Available

Cardiovascular Biology of the A3 Adenosine Receptor

Headrick, John P.; Peart, Jason N.; Wan, Tina C.; Kwok, Wai-Meng; Auchampach, John A.

Pages: 189 –208

[The goal of this chapter is to review current theories regarding the potential involvement of the A3 receptor in mediating the actions of adenosine in the cardiovascular system. The Gi protein-coupled A3 adenosine receptor is the last adenosine receptor subtype to be discovered and remains...

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