title: Emerging adenosine receptor agonists.
abstract: Adenosine receptors (ARs) are a four-member subfamily of G protein-coupled receptors and are major targets of caffeine and theophylline. There are four subtypes of ARs, designated as A1, A2A, A2B and A3. Selective agonists are now available for all four subtypes. Over a dozen of these selective agonists are now in clinical trials for various conditions, although none has received regulatory approval except for the endogenous AR agonist adenosine itself. A1AR agonists are in clinical trials for cardiac arrhythmias and neuropathic pain. A2AAR agonists are now in trials for myocardial perfusion imaging and as anti-inflammatory agents. A2BAR agonists are under preclinical scrutiny for potential treatment of cardiac ischemia. A3AR agonists are in clinical trials for the treatment of rheumatoid arthritis and colorectal cancer. The present review will mainly cover the agonists that are presently in clinical trials for various conditions and only a brief introduction will be given to major chemical classes of AR agonists presently under investigation.
authors.affiliation: NIDDK, 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
authors.forename: Zhan-Guo
authors.initials: ZG
authors.lastname: Gao
authors.forename: Kenneth A
authors.initials: KA
authors.lastname: Jacobson
mesh_terms: D000700:Analgesics / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000494:pharmacology; D018501:Antirheumatic Agents / Q000494:pharmacology; D002317:Cardiovascular Agents / Q000494:pharmacology; D015195:Drug Design; D015507:Drugs, Investigational / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D015394:Molecular Structure; D058906:Purinergic P1 Receptor Agonists; D016896:Treatment Outcome
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D018501:Antirheumatic Agents; D002317:Cardiovascular Agents; D015507:Drugs, Investigational; D058906:Purinergic P1 Receptor Agonists