Purinergic Receptors of the Central Nervous System: Biology, PET Ligands, and Their Applications.
paper
Cited
Public
- Authors
- Zarrinmayeh, Hamideh; Territo, Paul R
- Year
- 2020
- Journal
- Molecular imaging
- PMID
- 32539522
- DOI
- 10.1177/1536012120927609
- PMCID
- PMC7297484
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.
Purinergic receptor subfamilies and their endogenous ligands.
Structures of the adenosine A1 receptor [11C] PET radioligands: [11C]KF15372, [11C]MPDX, [11C]FR194921, and [11C]MMPD. PET indicates positron emission tomography.
Structures of the adenosine A1 receptor [18F] PET radioligands: [18F]CPFPX, [18F]CBCPM, and [18F]CPMMCB. PET indicates positron emission tomography.
Structures of the adenosine A2A receptor [11C] PET radioligands: [11C]TMSX, [11C]KF21213, [11C]SCH442416, and [11C]Preladenant. PET indicates positron emission tomography.
Structures of the adenosine A2A receptor [18F] PET radioligands: [18F]MRS5425 ([18F]-FESCH), [18F]-FPSCH, and [18F]MNI-444. PET indicates positron emission tomography.
Structures of the P2X7 receptor [11C] PET radioligands: [11C]A-740003, [11C]JNJ-54173717, [11C]GSK1482160, and [11C]SMW139. PET indicates positron emission tomography.
Structures of the P2X7 receptor [18F] PET radioligands: [18F]EFB, [18F]JNJ-64413739, and [18F]IUR-1601. PET indicates positron emission tomography.
[18F]Radiolabeled P2Y1R PET ligand [18F]18. PET indicates positron emission tomography.
[11C]Radiolabeled P2Y12R PET ligand [11C]5. PET indicates positron emission tomography.
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External
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| Altered purinergic receptor expression in the frontal cortex in schizophrenia. | Alnafisah R et al. | — | 2022 | → |
| Bidirectional Control between Cholesterol Shuttle and Purine Signal at the Central Nervous System. | Passarella D et al. | — | 2022 | → |
| Editorial: Purinergic signaling and neuroinflammation. | Assmann CE et al. | — | 2022 | → |
| Microglial Activation Modulated by P2X4R in Ischemia and Repercussions in Alzheimer's Disease. | Castillo C et al. | — | 2022 | → |
| Modulating brain integrative actions as a new perspective on pharmacological approaches to neuropsychiatric diseases. | Marcoli M et al. | — | 2022 | → |
| Multi-trait genome-wide association study of opioid addiction: OPRM1 and beyond. | Gaddis N et al. | — | 2022 | → |
| P2X receptor antagonists and their potential as therapeutics: a patent review (2010-2021). | Dane C et al. | — | 2022 | → |
| The impaired distribution of adenosine deaminase isoenzymes in multiple sclerosis plasma and cerebrospinal fluid. | Kutryb-Zajac B et al. | — | 2022 | → |
| The Multifaceted Role of GPCRs in Amyotrophic Lateral Sclerosis: A New Therapeutic Perspective? | Bassani D et al. | — | 2022 | → |
| The role of astrocytes in epileptic disorders. | Hayatdavoudi P et al. | — | 2022 | → |
| Adenosinergic Signaling as a Key Modulator of the Glioma Microenvironment and Reactive Astrocytes. | Debom GN et al. | — | 2021 | → |
| Development of <sup>18</sup>F-Labeled Radiotracers for PET Imaging of the Adenosine A<sub>2A</sub> Receptor: Synthesis, Radiolabeling and Preliminary Biological Evaluation. | Lai TH et al. | — | 2021 | → |
| Extracellular Vesicle Proteome of Breast Cancer Patients with and Without Cognitive Impairment Following Anthracycline-based Chemotherapy: An Exploratory Study. | Koh YQ et al. | — | 2021 | → |
| P2X<sub>7</sub> Receptors in Neurodegeneration: Potential Therapeutic Applications From Basic to Clinical Approaches. | Territo PR et al. | — | 2021 | → |
| P2Y<sub>2</sub> deficiency impacts adult neurogenesis and related forebrain functions. | Ali AAH et al. | — | 2021 | → |
| Role of microglia and P2X4 receptors in chronic pain. | Kohno K et al. | — | 2021 | → |
| Role of Purinergic Signaling in Acupuncture Therapeutics. | Lv ZY et al. | — | 2021 | → |
| Synthesis and Biological Evaluation of a Novel <sup>18</sup>F-Labeled Radiotracer for PET Imaging of the Adenosine A<sub>2A</sub> Receptor. | Lai TH et al. | — | 2021 | → |
| The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO. | Chen Z et al. | — | 2021 | → |
| Towards PET imaging of the dynamic phenotypes of microglia. | Beaino W et al. | — | 2021 | → |
| Purinergic signaling in infectious diseases of the central nervous system. | Alves VS et al. | — | 2020 | → |