Adenosine receptor targeting in health and disease.
BACKGROUND
The adenosine receptors A(1), A(2A), A(2B) and A(3) are important and ubiquitous mediators of cellular signaling that play vital roles in protecting tissues and organs from damage. In particular, adenosine triggers tissue protection and repair by different receptor-mediated mechanisms, including increasing the oxygen supply:demand ratio, pre-conditioning, anti-inflammatory effects and the stimulation of angiogenesis.


METHODS
The state of the art of the role of adenosine receptors which have been proposed as targets for drug design and discovery, in health and disease, and an overview of the ligands for these receptors in clinical development.


CONCLUSIONS
Selective ligands of A(1), A(2A), A(2B) and A(3) adenosine receptors are likely to find applications in the treatment of pain, ischemic conditions, glaucoma, asthma, arthritis, cancer and other disorders in which inflammation is a feature. The aim of this review is to provide an overview of the present knowledge regarding the role of these adenosine receptors in health and disease.
University of Ferrara, Department of Clinical and Experimental Medicine, Pharmacology Section, 44100 Ferrara, Italy.
Stefania
S
Gessi
Stefania
S
Merighi
Debora
D
Fazzi
Angela
A
Stefanelli
Katia
K
Varani
Pier Andrea
PA
Borea
D000241:Adenosine / Q000378:metabolism; D004194:Disease; D055808:Drug Discovery; D006262:Health; D006801:Humans; D058990:Molecular Targeted Therapy; D018047:Receptors, Purinergic P1 / Q000187:drug effects / Q000502:physiology*; D015398:Signal Transduction / Q000502:physiology
D018047:Receptors, Purinergic P1; D000241:Adenosine