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Purinergic Receptors of the Central Nervous System: Biology, PET Ligands, and Their Applications.
Molecular Imaging ( IF 2.2 ) Pub Date : 2020-06-15 , DOI: 10.1177/1536012120927609
Hamideh Zarrinmayeh 1 , Paul R Territo 1
Affiliation  

Purinergic receptors play important roles in central nervous system (CNS). These receptors are involved in cellular neuroinflammatory responses that regulate functions of neurons, microglial and astrocytes. Based on their endogenous ligands, purinergic receptors are classified into P1 or adenosine, P2X and P2Y receptors. During brain injury or under pathological conditions, rapid diffusion of extracellular adenosine triphosphate (ATP) or uridine triphosphate (UTP) from the damaged cells, promote microglial activation that result in the changes in expression of several of these receptors in the brain.

Imaging of the purinergic receptors with selective Positron Emission Tomography (PET) radioligands has advanced our understanding of the functional roles of some of these receptors in healthy and diseased brains. In this review, we have accumulated a list of currently available PET radioligands of the purinergic receptors that are used to elucidate the receptor functions and participations in CNS disorders. We have also reviewed receptors lacking radiotracer, laying the foundation for future discoveries of novel PET radioligands to reveal these receptors roles in CNS disorders.



中文翻译:

中枢神经系统的嘌呤能受体:生物学,PET配体及其应用。

嘌呤能受体在中枢神经系统(CNS)中起重要作用。这些受体参与调节神经元,小胶质细胞和星形胶质细胞功能的细胞神经炎症反应。根据其内源性配体,嘌呤能受体分为P1或腺苷,P2X和P2Y受体。在脑损伤期间或在病理条件下,细胞外三磷酸腺苷(ATP)或尿苷三磷酸(UTP)从受损细胞中迅速扩散,促进了小胶质细胞活化,导致大脑中这些受体中某些受体的表达发生变化。

用选择性正电子发射断层扫描(PET)放射性配体对嘌呤能受体进行成像,已经使我们对其中一些受体在健康和患病大脑中的功能作用有了更深入的了解。在这篇综述中,我们积累了嘌呤能受体的当前可用PET放射性配体的清单,这些清单可用于阐明受体功能和参与中枢神经系统疾病的情况。我们还审查了缺乏放射性示踪剂的受体,为将来发现新型PET放射性配体奠定基础,以揭示这些受体在中枢神经系统疾病中的作用。

更新日期:2020-06-30
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