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Adenosine A2A receptors, which have been cloned from several mammalian species, are activated by physiological concentrations of adenosine to stimulate the formation of cAMP and other mediators. The A2A receptors are found on neutrophil leukocytes, platelets, blood vessels and, very abundantly, on some cells in the CNS. In the caudate nucleus they coexist with dopamine D2 receptors, and stimulation of A2A receptors causes a decrease in D2 receptor-mediated neurotransmission. Thus, drugs that act on A2A receptors can be used to modify dopaminergic neurotransmission known to be important in neurological and psychiatric disorders. In this review, Ennio Ongini and Bertil Fredholm describe how recently developed potent and selective A2A receptor antagonists can be used to delineate the physiological and pathological processes regulated by A2A receptors. Results from in vitro and in vivo pharmacology studies strengthen the notion that A2A receptors are an interesting target for drug development.
E Ongini, and
B B Fredholm
January 2003,
Current topics in medicinal chemistry,
E Ongini, and
B B Fredholm
October 1997,
Annals of the New York Academy of Sciences,
E Ongini, and
B B Fredholm
January 2023,
International review of neurobiology,
E Ongini, and
B B Fredholm
January 2009,
Handbook of experimental pharmacology,
E Ongini, and
B B Fredholm
July 2006,
Blood,
E Ongini, and
B B Fredholm
February 2001,
Life sciences,
E Ongini, and
B B Fredholm
January 2018,
Frontiers in pharmacology,
E Ongini, and
B B Fredholm
November 2006,
Trends in neurosciences,
E Ongini, and
B B Fredholm
December 2007,
Progress in neurobiology,
