Authors: Holschbach, M.H.; Olsson, R.A.

Source: Current Pharmaceutical Design, Volume 8, Number 26, December 2002 , pp. 2345-2352(8)

Publisher: Bentham Science Publishers

Abstract:

In the last decade the field of purinergic pharmacology has continued to grow as the complexity of the receptor families and the various enzymes involved in purine metabolism have been defined in molecular terms. Adenosine receptors (ARs) are currently divided into the four subclasses A1-, A2A-, A2B- and A3AR. The most intensively studied subtypes are the high-affinity A1 and A2A receptors, which are activated by adenosine in nano- to submicromolar concentrations. The clinical importance of the A1 adenosine receptor (A1AR) and the A2A adenosine receptor (A2AAR) makes them attractive targets for radionuclide in vivo imaging. Positron Emission Tomography (PET) is an imaging modality which can determine biochemical and physiological processes in vivo in a quantitative way by using radiopharmaceuticals labeled with positron emitting radionuclides as 11C, 13N, 15O and 18F and by measuring the annihilation radiation using a coincidence technique. This includes also measurement of the pharmacokinetics of labeled drugs and the assessment of the effects of drugs on metabolism. In the present article we review the radioligands which are currently available for visualisation and quantification of ARs using PET with a special focus on the A1AR and A2AAR.

Keywords: adenosine receptor; adenosine ligands; positron emission tomography; ars; pet

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1381612023392955

Publication date: 2002-12-01

More about this publication?

• Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.
  
  Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.

Related content

• In this: publication
• By this: publisher
• In this Subject: Pharmacology
• By this author: Holschbach, M.H. ;  Olsson, R.A.

Website © Publishing Technology. Article copyright remains with the publisher, society or author(s) as specified within the article.

• Terms and conditions
• Privacy policy
• Information for advertisers