{"entity": "publication", "iuid": "68170984235543e3a87033df2cf1f668", "timestamp": "2026-09-06T15:18:50.882Z", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/68170984235543e3a87033df2cf1f668.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/68170984235543e3a87033df2cf1f668"}}, "title": "[18F]MK-7246 for Positron Emission Tomography Imaging of the Beta-Cell Surface Marker GPR44.", "authors": [{"family": "Cheung", "given": "Pierre", "initials": "P", "orcid": "0000-0003-1330-9800", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/2b8ff5c23c624f7b965e736f1f277c10.json"}}, {"family": "Amin", "given": "Mohammad A", "initials": "MA"}, {"family": "Zhang", "given": "Bo", "initials": "B", "orcid": "0000-0002-9199-1115", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/7ce4d3f145f14816a0c6f42481475c3a.json"}}, {"family": "Lechi", "given": "Francesco", "initials": "F"}, {"family": "Korsgren", "given": "Olle", "initials": "O", "orcid": "0000-0002-8524-9547", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/f4f384eeb31a4b2dba5c9301bb34c156.json"}}, {"family": "Eriksson", "given": "Jonas", "initials": "J"}, {"family": "Odell", "given": "Luke R", "initials": "LR"}, {"family": "Eriksson", "given": "Olof", "initials": "O", "orcid": "0000-0002-2515-8790", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/85991bf00e4b4a26ab15599d25c58601.json"}}], "type": "journal article", "published": "2023-02-02", "journal": {"title": "Pharmaceutics", "issn": "1999-4923", "volume": "15", "issue": "2", "issn-l": null}, "abstract": "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.", "doi": "10.3390/pharmaceutics15020499", "pmid": "36839820", "labels": {"SciLifeLab Fellow": null, "Olof Eriksson": null}, "xrefs": [{"db": "pmc", "key": "PMC9962486"}, {"db": "pii", "key": "pharmaceutics15020499"}], "notes": [], "created": "2023-05-14T14:50:44.384Z", "modified": "2023-05-14T14:50:44.482Z"}