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Potential Therapeutic Applications of Adenosine A 2A Receptor Ligands and Opportunities for A 2A Receptor Imaging
Author(s) -
Waarde Aren,
Dierckx Rudi A. J. O.,
Zhou Xiaoyun,
Khanapur Shivashankar,
Tsukada Hideo,
Ishiwata Kiichi,
Luurtsema Gert,
Vries Erik F. J.,
Elsinga Philip H.
Publication year - 2018
Publication title -
medicinal research reviews
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.868
H-Index - 130
eISSN - 1098-1128
pISSN - 0198-6325
DOI - 10.1002/med.21432
Subject(s) - adenosine a2a receptor , medicine , hippocampus , immunotherapy , immune system , neuroscience , positron emission tomography , adenosine receptor , striatum , rheumatoid arthritis , immunology , receptor , agonist , dopamine , psychology
Adenosine A 2A receptors (A 2A Rs) are highly expressed in the human striatum, and at lower densities in the cerebral cortex, the hippocampus, and cells of the immune system. Antagonists of these receptors are potentially useful for the treatment of motor fluctuations, epilepsy, postischemic brain damage, or cognitive impairment, and for the control of an immune checkpoint during immunotherapy of cancer. A 2A R agonists may suppress transplant rejection and graft‐versus‐host disease; be used to treat inflammatory disorders such as asthma, inflammatory bowel disease, and rheumatoid arthritis; be locally applied to promote wound healing and be employed in a strategy for transient opening of the blood–brain barrier (BBB) so that therapeutic drugs and monoclonal antibodies can enter the brain. Increasing A 2A R signaling in adipose tissue is also a potential strategy to combat obesity. Several radioligands for positron emission tomography (PET) imaging of A 2A Rs have been developed in recent years. This review article presents a critical overview of the potential therapeutic applications of A 2A R ligands, the use of A 2A R imaging in drug development, and opportunities and limitations of PET imaging in future research.