Bibliographic Details
| Title: |
[18F]MK-7246 for Positron Emission Tomography Imaging of the Beta-Cell Surface Marker GPR44 |
| Authors: |
Pierre Cheung, Mohammad A. Amin, Bo Zhang, Francesco Lechi, Olle Korsgren, Jonas Eriksson, Luke R. Odell, Olof Eriksson |
| Source: |
Pharmaceutics, Vol 15, Iss 2, p 499 (2023) |
| Publisher Information: |
MDPI AG, 2023. |
| Publication Year: |
2023 |
| Collection: |
LCC:Pharmacy and materia medica |
| Subject Terms: |
18F-labelling, beta-cell mass, diabetes, GPR44, CRTH2, islet imaging, Pharmacy and materia medica, RS1-441 |
| More Details: |
The progressive loss of beta-cell mass is a hallmark of diabetes and has been suggested as a complementary approach to studying the progression of diabetes in contrast to the beta-cell function. Non-invasive nuclear medicinal imaging techniques such as Positron Emission Tomography using radiation emitting tracers have thus been suggested as more viable methodologies to visualize and quantify the beta-cell mass with sufficient sensitivity. The transmembrane G protein-coupled receptor GPR44 has been identified as a biomarker for monitoring beta-cell mass. MK-7246 is a GPR44 antagonist that selectively binds to GPR44 with high affinity and good pharmacokinetic properties. Here, we present the synthesis of MK-7246, radiolabeled with the positron emitter fluorine-18 for preclinical evaluation using cell lines, mice, rats and human pancreatic cells. Here, we have described a synthesis and radiolabeling method for producing [18F]MK-7246 and its precursor compound. Preclinical assessments demonstrated the strong affinity and selectivity of [18F]MK-7246 towards GPR44. Additionally, [18F]MK-7246 exhibited excellent metabolic stability, a fast clearance profile from blood and tissues, qualifying it as a promising radioactive probe for GPR44-directed PET imaging. |
| Document Type: |
article |
| File Description: |
electronic resource |
| Language: |
English |
| ISSN: |
1999-4923 |
| Relation: |
https://www.mdpi.com/1999-4923/15/2/499; https://doaj.org/toc/1999-4923 |
| DOI: |
10.3390/pharmaceutics15020499 |
| Access URL: |
https://doaj.org/article/627424c53a45442bbbeb53570903b0a7 |
| Accession Number: |
edsdoj.627424c53a45442bbbeb53570903b0a7 |
| Database: |
Directory of Open Access Journals |
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