Publication

Potential Therapeutic Applications of Adenosine A2A Receptor Ligands and Opportunities for A2A Receptor Imaging

van Waarde, A., Dierckx, R. A. J. O., Zhou, X., Khanapur, S., Tsukada, H., Ishiwata, K., Luurtsema, G., de Vries, E. F. J. & Elsinga, P. H. Jan-2018 In : Medicinal research reviews. 38, 1, p. 5-56 52 p.

Research output: Scientific - peer-reviewReview article

Copy link to clipboard

Documents

  • Potential Therapeutic Applications of Adenosine A2A Receptor Ligands and Opportunities for A2A Receptor Imaging

    Final publisher's version, 722 KB, PDF-document

DOI

Adenosine A2A receptors (A2ARs) 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. A2AR 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 A2AR signaling in adipose tissue is also a potential strategy to combat obesity. Several radioligands for positron emission tomography (PET) imaging of A2ARs have been developed in recent years. This review article presents a critical overview of the potential therapeutic applications of A2AR ligands, the use of A2AR imaging in drug development, and opportunities and limitations of PET imaging in future research.

Original languageEnglish
Pages (from-to)5-56
Number of pages52
JournalMedicinal research reviews
Volume38
Issue number1
StatePublished - Jan-2018

    Keywords

  • Positron emission tomography (PET) imaging, adenosine A(2A) receptors, antagonists, agonists, drug development, POSITRON-EMISSION-TOMOGRAPHY, BLOOD-BRAIN-BARRIER, CENTRAL-NERVOUS-SYSTEM, EXPERIMENTAL AUTOIMMUNE ENCEPHALOMYELITIS, SPONTANEOUSLY HYPERTENSIVE-RATS, INFLAMMATORY-BOWEL-DISEASE, AMYGDALA-KINDLED SEIZURES, PERMANENT FOCAL ISCHEMIA, LUNG REPERFUSION INJURY, WORKING-MEMORY DEFICITS

View graph of relations

ID: 39474269