On the viability of tadalafil-based 18F-radiotracers for in vivo phosphodiesterase 5 (PDE5) PET imaging
Phosphodiesterase 5 (PDE5) is a clinically relevant biomarker and therapeutic target for many human pathologies, yet a noninvasive agent for the assessment of PDE5 expression has yet to be realized. Such agents would improve our understanding of the nitric oxide (NO)/cyclic guanosine 3′,5′-monophosp...
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| Hauptverfasser: | , , , , , , , |
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| Dokumenttyp: | Article (Journal) |
| Sprache: | Englisch |
| Veröffentlicht: |
12 August 2021
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| In: |
ACS omega
Year: 2021, Jahrgang: 6, Heft: 33, Pages: 21741-21754 |
| ISSN: | 2470-1343 |
| DOI: | 10.1021/acsomega.1c03315 |
| Online-Zugang: | Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1021/acsomega.1c03315
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| Verfasserangaben: | Justin J. Bailey, Melinda Wuest, Tamara Bojovic, Travis Kronemann, Carmen Wängler, Björn Wängler, Frank Wuest, and Ralf Schirrmacher |
MARC
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| 245 | 1 | 0 | |a On the viability of tadalafil-based 18F-radiotracers for in vivo phosphodiesterase 5 (PDE5) PET imaging |c Justin J. Bailey, Melinda Wuest, Tamara Bojovic, Travis Kronemann, Carmen Wängler, Björn Wängler, Frank Wuest, and Ralf Schirrmacher |
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| 520 | |a Phosphodiesterase 5 (PDE5) is a clinically relevant biomarker and therapeutic target for many human pathologies, yet a noninvasive agent for the assessment of PDE5 expression has yet to be realized. Such agents would improve our understanding of the nitric oxide (NO)/cyclic guanosine 3′,5′-monophosphate (cGMP)/PDE5 pathway in human pathologies and potentially lead to novel uses of PDE5 inhibitors to manage lung conditions like SARS-CoV-2-mediated pulmonary inflammatory responses. In this study, efforts were made to produce an 18F-labeled analogue of the PDE5 inhibitor tadalafil to visualize PDE5 expression in vivo with positron emission tomography (PET). However, during the late-stage fluorination step, quantitative epimerization of the tadalafil C12a stereocenter occurred, yielding a less active epi-isomer. In vivo dynamic microPET images in mice revealed that the epimerized radiotracer, [18F]epi-18, rapidly accumulated in the liver with negligible uptake in tissues of known PDE5 expression. | ||
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