In vivo evaluation of IGF1R/IR PET ligand [F]BMS-754807 in rodents.

Prabhakaran J, Dewey SL, McClure R, Simpson NR, Tantawy MN, Mann JJ, Pham W, Kumar JSD
Bioorg Med Chem Lett. 2017 27 (4): 941-943

PMID: 28094184 · PMCID: PMC5846678 · DOI:10.1016/j.bmcl.2016.12.086

In vivo evaluation of [F]BMS-754807 binding in mice and rats using microPET and biodistribution methods is described herein. The radioligand shows consistent binding characteristics, in vivo, in both species. Early time frames of the microPET images and time activity curves of brain indicate poor penetration of the tracer across the blood brain barrier (BBB) in both species. However, microPET experiments in mice and rats show high binding of the radioligand outside the brain to heart, pancreas and muscle, the organs known for higher expression of IGF1R/1R. Biodistribution analysis 2h after injection of [F]BMS-754807 in rats show negligible [F]defluorination as reflected by the low bone uptake and clearance from blood. Overall, the data indicate that [F]BMS-754807 can potentially be a radiotracer for the quantification of IGF1R/IR outside the brain using PET.

Copyright © 2017 Elsevier Ltd. All rights reserved.

MeSH Terms (12)

Animals Fluorine Radioisotopes Heterografts Humans Mice Positron-Emission Tomography Pyrazoles Radioligand Assay Rats Receptor, IGF Type 1 Receptor, Insulin Triazines

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