Synthesis, Radiolabeling, and in Vitro and in Vivo Evaluation of [18F]ENL30: A Potential PET Radiotracer for the 5-HT7 Receptor
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- acsomega.9b00394
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The 5-HT7 receptor (5-HT7R) is involved in a broad
range of physiological conditions and disorders. Currently, there is no
validated clinical positron emission tomography (PET) tracer available;
however, we have recently developed a promising 11C-labeled candidate. In this project, we aimed to further extend our efforts and develop an 18F-labeled derivative, coined [18F]ENL30.
Fluorine-18 has several advantages over carbon-11 especially within the
preclinical phase, where a long half-life usually increases evaluation
throughput. ENL30 was successfully synthesized in a low albeit
sufficient overall yield. Radiolabeling succeeded with a radiochemical
yield of approximately 4.5%. Subsequent preclinical PET studies revealed
that [18F]ENL30 binds specifically to the 5-HT7R but suffered from affinity to σ-receptors. Additionally, we identified [18F]ENL30 to be a P-gp substrate in rats. However, we believe that [18F]ENL30 may prove to be valuable in higher species that exhibit decreased P-gp
dependency. If required, σ-receptor binding could, in such studies, be
selectively blocked potentially allowing for selective 5-HT7R imaging.
Originalsprog | Engelsk |
---|---|
Tidsskrift | ACS Omega |
Vol/bind | 4 |
Udgave nummer | 4 |
Sider (fra-til) | 7344-7353 |
ISSN | 2470-1343 |
DOI | |
Status | Udgivet - 23 apr. 2019 |
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