In vivo evaluation of IGF1R/IR PET ligand [ 18 F]BMS-754807 in rodents

Content Provider	Scilit
Author	Prabhakaran, Jaya Dewey, Stephen L. McClure, Richard Simpson, Norman R. Tantawy, Mohammed N. Mann, J. John Pham, Wellington Kumar, J. S. Dileep
Copyright Year	2017
Description	Journal: Bioorganic & medicinal chemistry letters In vivo evaluation of [18F]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 [18F]BMS-754807 in rats show negligible [18F]defluorination as reflected by the low bone uptake and clearance from blood. Overall, the data indicate that [18F]BMS-754807 can potentially be a radiotracer for the quantification of IGF1R/IR outside the brain using PET.
Related Links	http://europepmc.org/articles/pmc5846678?pdf=render https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5846678/pdf
Ending Page	943
Page Count	3
Starting Page	941
ISSN	0960894X
DOI	10.1016/j.bmcl.2016.12.086
Journal	Bioorganic & medicinal chemistry letters
Issue Number	4
Volume Number	27
Language	English
Publisher	Elsevier BV
Publisher Date	2017-02-01
Access Restriction	Open
Subject Keyword	Journal: Bioorganic & medicinal chemistry letters Medicinal Chemistry
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Drug Discovery Biochemistry Molecular Biology Clinical Biochemistry Molecular Medicine Pharmaceutical Science