[18F]FMeNER-D2: A systematic in vitro analysis of radio-metabolism

Rami‐Mark, Christina; Eberherr, Nadine; Berroterán-Infante, Neydher; Vanicek, Thomas; Nics, Lukas; Lanzenberger, Rupert; Hacker, Marcus; Wadsak, Wolfgang; Mitterhauser, Markus

doi:10.1016/j.nucmedbio.2016.05.004

Cited by 6 publications

(2 citation statements)

References 19 publications

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“…In in vitro experiments, defluorination and subsequent binding to bone could not be confirmed. Possibly, some other metabolic degradation route is responsible for this phenomenon [24].…”

Section: Regions Of Interest (Rois)mentioning

confidence: 99%

Association of norepinephrine transporter methylation with in vivo NET expression and hyperactivity–impulsivity symptoms in ADHD measured with PET

et al. 2019

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Attention deficit hyperactivity disorder (ADHD) is a common neurodevelopmental disorder with a robust genetic influence. The norepinephrine transporter (NET) is of particular interest as it is one of the main targets in treatment of the disorder. As ADHD is a complex and polygenetic condition, the possible regulation by epigenetic processes has received increased attention. We sought to determine possible differences in NET promoter DNA methylation between patients with ADHD and healthy controls. DNA methylation levels in the promoter region of the NET were determined in 23 adult patients with ADHD and 23 healthy controls. A subgroup of 18 patients with ADHD and 18 healthy controls underwent positron emission tomography (PET) with the radioligand (S,S)-[ 18 F]FMeNER-D 2 to quantify the NET in several brain areas in vivo. Analyses revealed significant differences in NET methylation levels at several cytosine-phosphate-guanine (CpG) sites between groups. A defined segment of the NET promoter ("region 1") was hypermethylated in patients in comparison with controls. In ADHD patients, a negative correlation between methylation of a CpG site in this region and NET distribution in the thalamus, locus coeruleus, and the raphe nuclei was detected. Furthermore, methylation of several sites in region 1 was negatively associated with the severity of hyperactivity-impulsivity symptoms. Our results point to an epigenetic dysregulation in ADHD, possibly due to a compensatory mechanisms or additional factors involved in transcriptional processing.

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“…In in vitro experiments, defluorination and subsequent binding to bone could not be confirmed. Possibly, some other metabolic degradation route is responsible for this phenomenon [24].…”

Section: Regions Of Interest (Rois)mentioning

confidence: 99%

Association of norepinephrine transporter methylation with in vivo NET expression and hyperactivity–impulsivity symptoms in ADHD measured with PET

et al. 2019

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“…Die Menge an unverändertem Radiotracer (parent compound) wird über ein bestimmtes Zeitintervall bestimmt. Die Auswahl dieses Zeitfensters richtet sich nach der Halbwertszeit des Radionuklids, der Akquisitionsdauer und der Zeit bis zur Einstellung des Bindungsequilibriums an der Zielstruktur (time-to-equilibrium) [14][15][16]. Das Ausmaß des Metabolismus kann von Spezies zu Spezies variieren und ist bei höheren Spezies in der Regel weniger ausgeprägt oder langsamer (Gesetz von Kleiber) [17].…”

Section: Metabolismusunclassified

Perspektiven und Methoden der Experimentellen Nuklearmedizin

Balber

Mitterhauser

2021

Der Nuklearmediziner

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ZusammenfassungDie zentralen Aufgaben der experimentellen Nuklearmedizin liegen in der Entwicklung neuer Bildgebungsstrategien und Radioligandentherapien, in dem Erwerb eines tiefen molekularen Verständnisses für das Verhalten etablierter Radiopharmaka und der Entwicklung entsprechender Methodik für die Charakterisierung eben dieser. Die folgende Arbeit bietet einen Überblick über wichtige Parameter und Methoden der experimentellen Nuklearmedizin, die für die Realisierung einer erfolgreichen Bildgebungsstrategie und Radioligandentherapie essentiell sind.

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Recent advances in radiotracers targeting norepinephrine transporter: structural development and radiolabeling improvements

et al. 2020

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The norepinephrine transporter (NET) is a major target for the evaluation of the cardiac sympathetic nerve system in patients with heart failure and Parkinson's disease. It is also used in the therapeutic applications against certain types of neuroendocrine tumors, as exemplified by the clinically used 123/131 I-MIBG as theranostic single-photon emission computed tomography (SPECT) agent. With the development of more advanced positron emission tomography (PET) technology, more radiotracers targeting NET have been reported, with superior temporal and spatial resolutions, along with the possibility of functional and kinetic analysis. More recently, fluorine-18-labelled NET tracers have drawn increasing attentions from researchers, due to their longer radiological half-life relative to carbon-11 (110 min vs. 20 min), reduced dependence on on-site cyclotrons, and flexibility in the design of novel tracer structures. In the heart, certain NET tracers provide integral diagnostic information on sympathetic innervation and the nerve status. In the central nervous system, such radiotracers can reveal NET distribution and density in pathological conditions. Most radiotracers targeting cardiac NET-function for the cardiac application consistent of derivatives of either norepinephrine or MIBG with its benzylguanidine core structure, e.g. 11 C-HED and 18 F-LMI1195. In contrast, all NET tracers used in central nervous system applications are derived from clinically used antidepressants. Lastly, possible applications of NET as selective tracers over organic cation transporters (OCTs) in the kidneys and other organs controlled by sympathetic nervous system will also be discussed.

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[18F]FMeNER-D2: A systematic in vitro analysis of radio-metabolism

Cited by 6 publications

References 19 publications

Association of norepinephrine transporter methylation with in vivo NET expression and hyperactivity–impulsivity symptoms in ADHD measured with PET

Association of norepinephrine transporter methylation with in vivo NET expression and hyperactivity–impulsivity symptoms in ADHD measured with PET

Perspektiven und Methoden der Experimentellen Nuklearmedizin

Recent advances in radiotracers targeting norepinephrine transporter: structural development and radiolabeling improvements

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