Are A3 adenosine receptors expressed in the brain?

Scott A. Rivkees, Sundararajah Thevananther, Haiping Hao

Research output: Contribution to journalArticlepeer-review

65 Scopus citations


An increasing number of reports suggest a role for A3 adenosine receptors (A3ARs) in mediating adenosine action in the central nervous system. However, studies of A3AR localization in the brain have yet to be performed. To provide insights into the central sites of A3AR action, we compared patterns of A1 and A3AR mRNa and binding site expression in the brains of rats, mice and humans. We also assessed whether A3 agonists are selective for A3ARs. Whereas it was possible to detect high-level A1AR expression in many brain regions, it was not possible to detect either A3AR gene or binding site expression in the central nervous system. When we examined the affinities of the A3AR agonists CI-IAB-MECA and IAB-MECA for A1ARs, we found that these compounds bound to A1ARs with high affinity. These observations suggest that studies using A3-agonists need to consider potential effects of A1ARs activation, as A1ARs are abundantly expressed in the nervous system whereas A3AR expression in the brain cannot be directly demonstrated. (C) 2000 Lippincott Williams and Wilkins.

Original languageEnglish (US)
Pages (from-to)1025-1030
Number of pages6
Issue number5
StatePublished - Apr 7 2000
Externally publishedYes


  • Adenosine
  • Adenosine receptors
  • Brain
  • Testis

ASJC Scopus subject areas

  • General Neuroscience


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