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Related Experiment Videos

Emerging adenosine receptor agonists.

Zhan-Guo Gao1, Kenneth A Jacobson

  • 1NIDDK, National Institutes of Health, Molecular Recognition Section, Laboratory of Bioorganic Chemistry, Bldg. 8A, Room B1A-23, 9000 Rockville Pike, Bethesda, Maryland 20892-0810, USA. zg21o@nih.gov

Expert Opinion on Emerging Drugs
|September 19, 2007
PubMed
Summary
This summary is machine-generated.

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Selective agonists targeting adenosine receptors (ARs) are in clinical trials for numerous conditions, including pain, inflammation, and cancer. Research focuses on A1, A2A, A2B, and A3 subtypes, with potential therapeutic applications emerging.

Area of Science:

  • Pharmacology
  • Medicinal Chemistry
  • G protein-coupled receptors (GPCRs)

Background:

  • Adenosine receptors (ARs) comprise a four-member subfamily of GPCRs, targeted by compounds like caffeine and theophylline.
  • Selective agonists for all four AR subtypes (A1, A2A, A2B, A3) are now available.

Purpose of the Study:

  • To review selective AR agonists currently in clinical trials.
  • To provide an overview of major chemical classes of AR agonists under investigation.

Main Methods:

  • Literature review of AR agonists in clinical development.
  • Focus on agonists with selective activity at A1, A2A, A2B, and A3 receptors.

Main Results:

  • A1AR agonists are in trials for cardiac arrhythmias and neuropathic pain.

Related Experiment Videos

  • A2AAR agonists are investigated for myocardial perfusion imaging and anti-inflammatory effects.
  • A2BAR agonists show preclinical promise for cardiac ischemia; A3AR agonists are in trials for rheumatoid arthritis and colorectal cancer.

    • Conclusions:

    • Multiple selective AR agonists are progressing through clinical trials for diverse therapeutic indications.
    • While adenosine agonists are approved, further AR-targeted therapies are anticipated.