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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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Main Authors: Bailey, Justin (Author) , Wuest, Melinda (Author) , Bojovic, Tamara (Author) , Kronemann, Travis (Author) , Wängler, Carmen (Author) , Wängler, Björn (Author) , Wuest, Frank (Author) , Schirrmacher, Ralf (Author)
Format: Article (Journal)
Language:English
Published: 12 August 2021
In: ACS omega
Year: 2021, Volume: 6, Issue: 33, Pages: 21741-21754
ISSN:2470-1343
DOI:10.1021/acsomega.1c03315
Online Access:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1021/acsomega.1c03315
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Author Notes:Justin J. Bailey, Melinda Wuest, Tamara Bojovic, Travis Kronemann, Carmen Wängler, Björn Wängler, Frank Wuest, and Ralf Schirrmacher
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Summary: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.
Item Description:Im Titel ist "18" hochgestellt
Published online 12 August 2021
Gesehen am 06.12.2022
Physical Description:Online Resource
ISSN:2470-1343
DOI:10.1021/acsomega.1c03315

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