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

Author(s):
Verbeek, J.; Eriksson, J.; Syvänen, S.; Huisman, M.; Schuit, R.C.; Molthoff, C.F.M.; Voskuyl, R.A.; Lange, E.C.M. de (0000-0001-8303-1117); Lammertsma, A.A.; Windhorst, A.D.
Published
2018
Publication type
Article / Letter to editor

Abstract

-(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.

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.

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.

Background Results Conclusion

Date issued
2018-12-31
Language
English
Is part of
EJNMMI Radiopharmacy and Chemistry (2018), Vol. 3, p. 11
hdl
1887/70716
doi
10.1186/s41181-018-0046-z