Emerging adenosine receptor agonists – an update

Abstract

Adenosine receptors (ARs), the major targets of caffeine and theophylline, comprise four receptor subtypes designated as A₁, A_2A, A_2B and A₃. Over a dozen AR agonists are currently in clinical trials for various conditions, including cardiac arrhythmias, neuropathic pain, myocardial perfusion imaging, cardiac ischemia, inflammatory diseases and cancer. Adenosine (nonselective), regadenoson (A_2A) and dipyridamole (act indirectly via ARs) have received regulatory approval for clinical use. The present editorial will give a brief update on the current status of AR agonists in clinical trials.

Keywords:

• adenosine receptor
• agonist
• cancer
• cardiac arrhythmia
• cardiac perfusion imaging
• G-protein-coupled receptor
• inflammation
• nucleoside
• pain
• rheumatoid arthritis