Literature DB >> 24059232

Adenosine A(2A) receptor antagonists as Positron Emission Tomography (PET) tracers.

S Khanapur, A van Waarde, K Ishiwata, K L Leenders, R A J O Dierckx, P H Elsinga1.   

Abstract

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.

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Year:  2014        PMID: 24059232     DOI: 10.2174/09298673113206660265

Source DB:  PubMed          Journal:  Curr Med Chem        ISSN: 0929-8673            Impact factor:   4.530


  6 in total

Review 1.  The Role of Adenosine Tone and Adenosine Receptors in Huntington's Disease.

Authors:  David Blum; Yijuang Chern; Maria Rosaria Domenici; Luc Buée; Chien-Yu Lin; William Rea; Sergi Ferré; Patrizia Popoli
Journal:  J Caffeine Adenosine Res       Date:  2018-06-01

2.  PET Imaging of the Adenosine A2A Receptor in the Rotenone-Based Mouse Model of Parkinson's Disease with [18F]FESCH Synthesized by a Simplified Two-Step One-Pot Radiolabeling Strategy.

Authors:  Susann Schröder; Thu Hang Lai; Magali Toussaint; Mathias Kranz; Alexandra Chovsepian; Qi Shang; Sladjana Dukić-Stefanović; Winnie Deuther-Conrad; Rodrigo Teodoro; Barbara Wenzel; Rareş-Petru Moldovan; Francisco Pan-Montojo; Peter Brust
Journal:  Molecules       Date:  2020-04-02       Impact factor: 4.411

Review 3.  Molecular probes for the human adenosine receptors.

Authors:  Xue Yang; Laura H Heitman; Adriaan P IJzerman; Daan van der Es
Journal:  Purinergic Signal       Date:  2020-12-12       Impact factor: 3.765

Review 4.  In Vivo Positron Emission Tomography Imaging of Adenosine A2A Receptors.

Authors:  Meng-Juan Sun; Fang Liu; Ya-Fei Zhao; Xiao-Ai Wu
Journal:  Front Pharmacol       Date:  2020-11-26       Impact factor: 5.810

5.  Single Stabilizing Point Mutation Enables High-Resolution Co-Crystal Structures of the Adenosine A2A Receptor with Preladenant Conjugates.

Authors:  Tobias Claff; Tim A Klapschinski; Udaya K Tiruttani Subhramanyam; Victoria J Vaaßen; Jonathan G Schlegel; Christin Vielmuth; Jan H Voß; Jörg Labahn; Christa E Müller
Journal:  Angew Chem Int Ed Engl       Date:  2022-03-24       Impact factor: 16.823

Review 6.  Evidence of inflammatory system involvement in Parkinson's disease.

Authors:  Yinxia Chao; Siew Cheng Wong; Eng King Tan
Journal:  Biomed Res Int       Date:  2014-06-24       Impact factor: 3.411

  6 in total

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