2008/06/06 by John W. Daly, Izumi Hide, Christa E. M uuml ller +1 · 1 citation
Biochemistry, Genetics and Molecular Biology · Engineering · Chemistry · #Adenosine and Purinergic Signaling #Organic Light-Emitting Diodes Research #Synthesis and Biological Evaluation
paper · doi:10.1159/000138813
openalex publication_date 2008/06/06 · openalex created_date 2025/10/10 · openalex updated_date 2026/07/31
Caffeine and analogs that contain ethyl, propyl, allyl, propargyl and other substituents in place of methyl at 1-, 3- and 7-positions were antagonists at the two major classes (A1 and A2) of adenosine receptors. Potency at both receptors increased as methyls were replaced with larger substituents. Certain analogs with only one of the three methyl groups of caffeine replaced by larger substituents were somewhat selective for A2 receptors. None of the analogs were particularly selective for A1 receptors. The presence of polar entities in the substituent at the 1- or 7-position was poorly tolerated at adenosine receptors. Activity of caffeine analogs at A1 and A2 adenosine receptors in a variety of systems and cell types is presented and summarized.