Adenosine A2A Receptor Antagonists as Positron Emission Tomography (PET) Tracers

被引：0
作者：
Khanapur, S. [1 ]
van Waarde, A. [1 ]
Ishiwata, K. [2 ]
Leenders, K. L. [4 ]
Dierckx, R. A. J. O. [1 ,3 ]
Elsinga, P. H. [1 ,3 ]
机构：
[1] Univ Groningen, Univ Med Ctr Groningen, NL-9713 GZ Groningen, Netherlands
[2] Tokyo Metropolitan Inst Gerontol, Positron Med Ctr, Tokyo, Japan
[3] Univ Hosp Ghent, Dept Nucl Med, Ghent, Belgium
[4] Univ Groningen, Univ Med Ctr Groningen, Dept Neurol, NL-9713 GZ Groningen, Netherlands
来源：
CURRENT MEDICINAL CHEMISTRY | 2014年 / 21卷 / 03期
关键词：
Adenosine A(2A) receptor; Parkinson's disorder; positron emission tomography (PET); xanthine ligands; nonxanthine; ligands; SCH442416; TMSX; 6-OHDA PD model; MOVEMENT-DISORDER SOCIETY; CENTRAL-NERVOUS-SYSTEM; JOINT TASK-FORCE; PARKINSONS-DISEASE; THERAPEUTIC MANAGEMENT; PIPERAZINE DERIVATIVES; NEUROLOGICAL SOCIETIES; MEDICINAL CHEMISTRY; EUROPEAN FEDERATION; SELECTIVE LIGAND;
D O I：
暂无
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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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收藏
页码：312 / 328
页数：17
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