Synthesis and preliminary preclinical evaluation of fluorine-18 labelled isatin-4-(4-methoxyphenyl)-3-thiosemicarbazone ([18F]4FIMPTC) as a novel PET tracer of P-glycoprotein expression

Verbeek, J.; Eriksson, J.; Syvänen, S.; Huisman, M.; Schuit, R.C.; Molthoff, C.F.M.; ... ; Windhorst, A.D. (2018)

Article / Letter to editor

-(4-methoxyphenyl)hydrazine-carbothioamide was described as a potential selective P-gp inhibitor that is not transported by P-gp. Therefore, the purpose of this study was to radiolabel two of its analogues and to assess their potential for imaging P-gp expression using PET.\n across the blood-brain barrier was not altered by pre-treatment with the P-gp inhibitor tariquidar, and uptake was significantly lower in P-gp KO than in wild-type animals and indeed transported across the BBB or bound to P-gp in endothelial cells.\n appears to be a radiotracer that binds to P-gp, as showed in P-gp knock-out animals, but is not a substrate for P-gp.\nBackground\nResults\nConclusion

• All authors: Verbeek, J.; Eriksson, J.; Syvänen, S.; Huisman, M.; Schuit, R.C.; Molthoff, C.F.M.; Voskuyl, R.A.; Lange, E.C.M. de; Lammertsma, A.A.; Windhorst, A.D.
• Date: 2018-12-31
• Journal: EJNMMI Radiopharmacy and Chemistry
• Volume: 3
• Pages: 11
• DOI: doi:10.1186/s41181-018-0046-z