Title:Potential Therapeutic Relevance of Adenosine A2B and A2A Receptors in the Central Nervous System
Volume: 11
Issue: 6
Author(s): Patrizia Popoli and Rita Pepponi
Affiliation:
Keywords:
Adenosine A2B receptors, adenosine A2A receptors, Central Nervous System, drug target, neurodegeneration,
neuroprotection, Adenosine A2B receptors, adenosine A2A receptors, Central Nervous System, drug target, neurodegeneration, neuroprotection, A2AR, A2BR, Alzheimer’s disease, Brain derived neurotrophic factor,
Abstract: Adenosine A2B and, much more importantly, adenosine A2A receptors modulate many physiological and
pathological processes in the brain. In this review, the most recent evidence concerning the role of such receptors and their
potential therapeutic relevance is discussed. The low affinity of A2B receptors for adenosine implies that they might
represent a good therapeutic target, since they are activated only under pathological conditions (when adenosine levels
raise up to micromolar concentrations). The availability of selective ligands for A2B receptors would allow exploration of
such an hypothesis. Since adenosine A2A receptors mediate both potentially neuroprotective and potentially neurotoxic
effects, their role in neurodegenerative diseases is highly controversial. Nevertheless, A2A receptor antagonists have
shown clear antiparkinsonian effects, and a great interest exists on the role of A2A receptors in Alzheimer’s disease, brain
ischaemia, spinal cord injury, drug addiction and other conditions. In order to establish whether such receptors represent a
target for CNS diseases, at least two conditions are needed: the full comprehension of A2A-dependent mechanisms and the
availability of ligands capable of discriminating among the different receptor populations.
