Adenosine receptors in the central nervous system: Relationship to the central actions of methylxanthines

John W. Daly, Robert F. Bruns, S. H. Snyder

Research output: Contribution to journalArticlepeer-review

Abstract

Adenosine has a significant role in many functions of the central nervous system. Behaviorally, adenosine and adenosine analogs have marked depressant effects. Electrophysiologically, adenosine reduces spontaneous neuronal activity and inhibits transsynaptic potentials via interaction with extracellular receptors. Biochemically, adenosine inhibits adenylate cyclase via a "high" affinity receptor, and activates adenylate cyclase via a "low" affinity receptor. These receptors, called "A1" and "A2" respectively, show differing profiles for activation by adenosine analogs. Radioactive N6-cyclohexyladenosine binds selectively to the "high" affinity receptor. One major class of antagonists is known at adenosine receptors: the alkylxanthines, including caffeine and theophylline. Radioactive 1,3-diethyl-8-phenylxanthine, a particularly potent antagonist, appears to bind to both low and high affinity adenosine receptors. Behavioral, electrophysiological, and biochemical effects of alkylxanthines are consistent with the hypothesis that the central stimulatory actions of caffeine and theophylline are due in large part to antagonism of central adenosine receptors.

Original languageEnglish (US)
Pages (from-to)2083-2097
Number of pages15
JournalLife Sciences
Volume28
Issue number19
DOIs
StatePublished - May 11 1981

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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