In vivo imaging of brain androgen receptors in rats: a [(18)F]FDHT PET study

Nuclear Medicine and Biology
M A KhayumErik F J de Vries

Abstract

Steroid hormones like androgens play an important role in the development and maintenance of several brain functions. Androgens can act through androgen receptors (AR) in the brain. This study aims to demonstrate the feasibility of positron emission tomography (PET) with 16β-[(18)F]fluoro-5α-dihydrotestosterone ([(18)F]FDHT) to image AR expression in the brain. Male Wistar rats were either orchiectomized to inhibit endogenous androgen production or underwent sham-surgery. Fifteen days after surgery, rats were subjected to a 90-min dynamic [(18)F]FDHT PET scan with arterial blood sampling. In a subset of orchiectomized rats, 1mg/kg dihydrotestosterone was co-injected with the tracer in order to saturate the AR. Plasma samples were analyzed for the presence of radioactive metabolites by radio-TLC. Pharmacokinetic modeling was performed to quantify brain kinetics of the tracer. After the PET scan, the animals were terminated for ex-vivo biodistribution. PET imaging and ex vivo biodistribution studies showed low [(18)F]FDHT uptake in all brain regions, except pituitary. [(18)F]FDHT uptake in the surrounding cranial bones was high and increased over time. [(18)F]FDHT was rapidly metabolized in rats. Metabolism was significantly fast...Continue Reading

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Citations

Jul 30, 2016·Frontiers in Oncology·Natalie J Serkova, S Gail Eckhardt
Dec 14, 2017·Journal of Neuroendocrinology·R Moraga-AmaroE F J de Vries
Dec 3, 2020·Cancer Research·Natalie J SerkovaRalph P Mason
Jun 2, 2018·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Benjamin M LarimerUmar Mahmood
Feb 1, 2021·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Inês F AntunesIgle J de Jong

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