Update on PET Tracer Development for Muscarinic Acetylcholine Receptors
The muscarinic cholinergic system regulates peripheral and central nervous system functions, and, thus, their potential as a therapeutic target for several neurodegenerative diseases is undoubted. A clinically applicable positron emission tomography (PET) tracer would facilitate the monitoring of di...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-06-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/14/6/530 |
| _version_ | 1797531575760453632 |
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| author | Marius Ozenil Jonas Aronow Marlon Millard Thierry Langer Wolfgang Wadsak Marcus Hacker Verena Pichler |
| author_facet | Marius Ozenil Jonas Aronow Marlon Millard Thierry Langer Wolfgang Wadsak Marcus Hacker Verena Pichler |
| author_sort | Marius Ozenil |
| collection | DOAJ |
| description | The muscarinic cholinergic system regulates peripheral and central nervous system functions, and, thus, their potential as a therapeutic target for several neurodegenerative diseases is undoubted. A clinically applicable positron emission tomography (PET) tracer would facilitate the monitoring of disease progression, elucidate the role of muscarinic acetylcholine receptors (mAChR) in disease development and would aid to clarify the diverse natural functions of mAChR regulation throughout the nervous system, which still are largely unresolved. Still, no mAChR PET tracer has yet found broad clinical application, which demands mAChR tracers with improved imaging properties. This paper reviews strategies of mAChR PET tracer design and summarizes the binding properties and preclinical evaluation of recent mAChR tracer candidates. Furthermore, this work identifies the current major challenges in mAChR PET tracer development and provides a perspective on future developments in this area of research. |
| first_indexed | 2024-03-10T10:45:46Z |
| format | Article |
| id | doaj.art-4e539dbef7d242ffa9f625507d05556e |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-10T10:45:46Z |
| publishDate | 2021-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-4e539dbef7d242ffa9f625507d05556e2023-11-21T22:35:12ZengMDPI AGPharmaceuticals1424-82472021-06-0114653010.3390/ph14060530Update on PET Tracer Development for Muscarinic Acetylcholine ReceptorsMarius Ozenil0Jonas Aronow1Marlon Millard2Thierry Langer3Wolfgang Wadsak4Marcus Hacker5Verena Pichler6Department of Biomedical Imaging and Image-Guided Therapy, Medical University of Vienna, 1090 Wien, AustriaDepartment of Biomedical Imaging and Image-Guided Therapy, Medical University of Vienna, 1090 Wien, AustriaDepartment of Pharmaceutical Sciences, Division of Pharmaceutical Chemistry, University of Vienna, 1090 Wien, AustriaDepartment of Pharmaceutical Sciences, Division of Pharmaceutical Chemistry, University of Vienna, 1090 Wien, AustriaDepartment of Biomedical Imaging and Image-Guided Therapy, Medical University of Vienna, 1090 Wien, AustriaDepartment of Biomedical Imaging and Image-Guided Therapy, Medical University of Vienna, 1090 Wien, AustriaDepartment of Pharmaceutical Sciences, Division of Pharmaceutical Chemistry, University of Vienna, 1090 Wien, AustriaThe muscarinic cholinergic system regulates peripheral and central nervous system functions, and, thus, their potential as a therapeutic target for several neurodegenerative diseases is undoubted. A clinically applicable positron emission tomography (PET) tracer would facilitate the monitoring of disease progression, elucidate the role of muscarinic acetylcholine receptors (mAChR) in disease development and would aid to clarify the diverse natural functions of mAChR regulation throughout the nervous system, which still are largely unresolved. Still, no mAChR PET tracer has yet found broad clinical application, which demands mAChR tracers with improved imaging properties. This paper reviews strategies of mAChR PET tracer design and summarizes the binding properties and preclinical evaluation of recent mAChR tracer candidates. Furthermore, this work identifies the current major challenges in mAChR PET tracer development and provides a perspective on future developments in this area of research.https://www.mdpi.com/1424-8247/14/6/530molecular imagingPETtracer developmentmuscarinic acetylcholine receptors |
| spellingShingle | Marius Ozenil Jonas Aronow Marlon Millard Thierry Langer Wolfgang Wadsak Marcus Hacker Verena Pichler Update on PET Tracer Development for Muscarinic Acetylcholine Receptors Pharmaceuticals molecular imaging PET tracer development muscarinic acetylcholine receptors |
| title | Update on PET Tracer Development for Muscarinic Acetylcholine Receptors |
| title_full | Update on PET Tracer Development for Muscarinic Acetylcholine Receptors |
| title_fullStr | Update on PET Tracer Development for Muscarinic Acetylcholine Receptors |
| title_full_unstemmed | Update on PET Tracer Development for Muscarinic Acetylcholine Receptors |
| title_short | Update on PET Tracer Development for Muscarinic Acetylcholine Receptors |
| title_sort | update on pet tracer development for muscarinic acetylcholine receptors |
| topic | molecular imaging PET tracer development muscarinic acetylcholine receptors |
| url | https://www.mdpi.com/1424-8247/14/6/530 |
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