Publication

Adenosine A(2A) Receptor Antagonists as Positron Emission Tomography (PET) Tracers

Khanapur, S., van Waarde, A., Ishiwata, K., Leenders, K. L., Dierckx, R. A. J. O. & Elsinga, P. H., Jan-2014, In : CURRENT MEDICINAL CHEMISTRY. 21, 3, p. 312-328 17 p.

Research output: Contribution to journalArticleAcademicpeer-review

The adenosine A(2A) receptor (A(2A)R) is highly concentrated in the striatum, and a therapeutic target for Parkinson's disorder (PD) and Huntington's disease. High affinity and selective radiolabeled A(2A)R antagonists can be important research and diagnostic tools for PD. Positron Emission Tomography (PET) can play an important role by measuring radiolabeled A(2A) antagonists non-invasively in the brain. However, till date no complete review on A(2A)R PET ligands is available. The present article has been therefore focused on available PET tracers for A(2A)R and their detailed biological evaluation in rodents, nonhuman primates and humans. Drug design and development by molecular modeling including new lead structures that are potential candidates for radiolabeling and mapping of cerebral A(2A)Rs is discussed in the present article. A brief overview of functions of adenosine in health and disease, including the relevance of A(2A)R for PD has also been presented.

Original languageEnglish
Pages (from-to)312-328
Number of pages17
JournalCURRENT MEDICINAL CHEMISTRY
Volume21
Issue number3
Publication statusPublished - Jan-2014

    Keywords

  • Adenosine A(2A) receptor, Parkinson's disorder, positron emission tomography (PET), xanthine ligands, nonxanthine, ligands, SCH442416, TMSX, 6-OHDA PD model, CENTRAL-NERVOUS-SYSTEM, MOVEMENT-DISORDER SOCIETY, JOINT TASK-FORCE, PARKINSONS-DISEASE, RAT-BRAIN, THERAPEUTIC MANAGEMENT, PIPERAZINE DERIVATIVES, NEUROLOGICAL SOCIETIES, MEDICINAL CHEMISTRY, EUROPEAN FEDERATION

ID: 13706062