Academic literature on the topic 'Radiometabolites'

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Journal articles on the topic "Radiometabolites"

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Tonietto, Matteo, Gaia Rizzo, Mattia Veronese, et al. "Plasma radiometabolite correction in dynamic PET studies: Insights on the available modeling approaches." Journal of Cerebral Blood Flow & Metabolism 36, no. 2 (2015): 326–39. http://dx.doi.org/10.1177/0271678x15610585.

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Full kinetic modeling of dynamic PET images requires the measurement of radioligand concentrations in the arterial plasma. The unchanged parent radioligand must, however, be separated from its radiometabolites by chromatographic methods. Thus, only few samples can usually be analyzed and the resulting measurements are often noisy. Therefore, the measurements must be fitted with a mathematical model. This work presents a comprehensive analysis of the different models proposed in the literature to describe the plasma parent fraction (PPf) and of the alternative approaches for radiometabolite cor
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Nag, Sangram, Ryosuke Arakawa, Zhisheng Jia, et al. "Characterization of a Novel M4 PAM PET Radioligand [11C]PF06885190 in Nonhuman Primates (NHP)." Molecules 28, no. 12 (2023): 4612. http://dx.doi.org/10.3390/molecules28124612.

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Muscarinic acetylcholine receptors (mAChR), including M4, draw attention as therapeutic targets for several neurodegenerative diseases including Alzheimer’s disease (AD). PET imaging of M4 positive allosteric modulator (PAM) allows qualification of the distribution as well as the expression of this receptor under physiological conditions and thereby helps to assess the receptor occupancy (RO) of a drug candidate. In this study, our aims were (a) to synthesize a novel M4 PAM PET radioligand [11C]PF06885190 (b) to evaluate the brain distribution of [11C]PF06885190 in nonhuman primates (NHP) and
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Johansen, Annette, Hanne D. Hansen, Claus Svarer, et al. "The importance of small polar radiometabolites in molecular neuroimaging: A PET study with [11C]Cimbi-36 labeled in two positions." Journal of Cerebral Blood Flow & Metabolism 38, no. 4 (2017): 659–68. http://dx.doi.org/10.1177/0271678x17746179.

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[11C]Cimbi-36, a 5-HT2A receptor agonist PET radioligand, contains three methoxy groups amenable to [11C]-labeling. In pigs, [11C]Cimbi-36 yields a polar (M1) and a less polar (M2) radiometabolite fraction, while changing the labeling to [11C]Cimbi-36_5 yields only the M1 fraction. We investigate whether changing the labeling position of [11C]Cimbi-36 eliminates M2 in humans, and if this changes the signal-to-background ratio. Six healthy volunteers each underwent two dynamic PET scans; after injection of [11C]Cimbi-36, both the M1 and M2 fraction appeared in plasma, whereas only the M1 appear
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Tonietto, Matteo, Mattia Veronese, Gaia Rizzo, et al. "Improved Models for Plasma Radiometabolite Correction and their Impact on Kinetic Quantification in PET Studies." Journal of Cerebral Blood Flow & Metabolism 35, no. 9 (2015): 1462–69. http://dx.doi.org/10.1038/jcbfm.2015.61.

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The quantification of dynamic positron emission tomography studies performed with arterial sampling usually requires correcting the input function for the presence of radiometabolites by using a model of the plasma parent fraction (PPf). Here, we show how to include the duration of radioligand injection in the PPf model formulations to achieve a more physiologic description of the plasma measurements. This formulation (here called convoluted model) was tested on simulated data and on three datasets with different parent kinetics: [11C]NOP-1A, [11C]MePPEP, and [11C](R)-rolipram. Results showed
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Auvity, Sylvain, Louise Breuil, Maud Goislard, et al. "An original radio-biomimetic approach to synthesize radiometabolites for PET imaging." Nuclear Medicine and Biology 90-91 (November 2020): 10–14. http://dx.doi.org/10.1016/j.nucmedbio.2020.08.001.

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Klebermass, Eva-Maria, Mahshid Mahmudi, Barbara Katharina Geist, et al. "If It Works, Don’t Touch It? A Cell-Based Approach to Studying 2-[18F]FDG Metabolism." Pharmaceuticals 14, no. 9 (2021): 910. http://dx.doi.org/10.3390/ph14090910.

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The glucose derivative 2-[18F]fluoro-2-deoxy-D-glucose (2-[18F]FDG) is still the most used radiotracer for positron emission tomography, as it visualizes glucose utilization and energy demand. In general, 2-[18F]FDG is said to be trapped intracellularly as 2-[18F]FDG-6-phosphate, which cannot be further metabolized. However, increasingly, this dogma is being questioned because of publications showing metabolism beyond 2-[18F]FDG-6-phosphate and even postulating 2-[18F]FDG imaging to depend on the enzyme hexose-6-phosphate dehydrogenase in the endoplasmic reticulum. Therefore, we aimed to study
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Lai, Thu Hang, Magali Toussaint, Rodrigo Teodoro, et al. "Improved in vivo PET imaging of the adenosine A2A receptor in the brain using [18F]FLUDA, a deuterated radiotracer with high metabolic stability." European Journal of Nuclear Medicine and Molecular Imaging 48, no. 9 (2021): 2727–36. http://dx.doi.org/10.1007/s00259-020-05164-4.

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Abstract Purpose The adenosine A2A receptor has emerged as a therapeutic target for multiple diseases, and thus the non-invasive imaging of the expression or occupancy of the A2A receptor has potential to contribute to diagnosis and drug development. We aimed at the development of a metabolically stable A2A receptor radiotracer and report herein the preclinical evaluation of [18F]FLUDA, a deuterated isotopologue of [18F]FESCH. Methods [18F]FLUDA was synthesized by a two-step one-pot approach and evaluated in vitro by autoradiographic studies as well as in vivo by metabolism and dynamic PET/MRI
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Wenzel, Barbara, Stefan R. Fritzsche, Magali Toussaint, et al. "Radiosynthesis and Preclinical Evaluation of an 18F-Labeled Triazolopyridopyrazine-Based Inhibitor for Neuroimaging of the Phosphodiesterase 2A (PDE2A)." Pharmaceuticals 15, no. 10 (2022): 1272. http://dx.doi.org/10.3390/ph15101272.

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The cyclic nucleotide phosphodiesterase 2A is an intracellular enzyme which hydrolyzes the secondary messengers cAMP and cGMP and therefore plays an important role in signaling cascades. A high expression in distinct brain areas as well as in cancer cells makes PDE2A an interesting therapeutic and diagnostic target for neurodegenerative and neuropsychiatric diseases as well as for cancer. Aiming at specific imaging of this enzyme in the brain with positron emission tomography (PET), a new triazolopyridopyrazine-based derivative (11) was identified as a potent PDE2A inhibitor (IC50, PDE2A = 1.9
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Nag, Sangram, Patrik Fazio, Lutz Lehmann, et al. "In Vivo/In Vitro Characterisation of a Novel MAO-B Inhibitor Radioligand, Fluorine-18 Labeled Deuterated Fluorodeprenyl (18F-Fluorodeprenyl-D2)." Journal of Nuclear Medecine 57, no. 2 (2015): 315–20. https://doi.org/10.2967/jnumed.115.161083.

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INTRODUCTION: The aim of this study was to radiolabel a novel bis-deuterium substituted L-deprenyl analogue (<sup>18</sup>F-fluorodeprenyl-D<sub>2</sub>) with fluorine-18 and to evaluate its potential to visualize and quantify monoamine oxidase B (MAO-B) activity in vivo. METHODS: The precursor compound (5a + 5b) and reference standard (6) were synthesized in multi-step syntheses. Recombinant human MAO-B and MAO-A enzyme preparations were used in order to determine IC50 values. Radiolabeling was accomplished by nucleophilic substitution reaction. Whole hemisphere autoradiography (ARG) was perf
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Samén, Erik, Jan-Olov Thorell, Anna Fredriksson, and Sharon Stone-Elander. "The tyrosine kinase inhibitor PD153035: implication of labeling position on radiometabolites formed in vitro." Nuclear Medicine and Biology 33, no. 8 (2006): 1005–11. http://dx.doi.org/10.1016/j.nucmedbio.2006.09.008.

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Dissertations / Theses on the topic "Radiometabolites"

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Tonietto, Matteo. "A Unified Framework For Blood Data Modeling In Dynamic Positron Emission Tomography Studies." Doctoral thesis, Università degli studi di Padova, 2017. http://hdl.handle.net/11577/3424684.

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Quantification of dynamic PET images requires the measurement of radioligand concentrations in the arterial plasma. In general, this cannot be derived from PET images directly but it must be measured from blood samples taken from the subject’s radial artery. The aim of this thesis was to develop and validate a unified framework for the blood data modeling, which was both biologically and experimentally informed, in order to achieve a better description of the blood data.<br>La quantificazione di immagini dinamiche PET (Tomografia ad Emissione di Positroni) richiede la misurazione della con
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Link, Jeanne Meyers. "Mixed-mode chromatographic separation and whole column radiation detection to improve sensitivity in radiometabolite analysis : application to (Carbon-11)-meta-hydroxyephedrine in plasma /." Thesis, Connect to this title online; UW restricted, 1998. http://hdl.handle.net/1773/8578.

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Book chapters on the topic "Radiometabolites"

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Cohen, Yves, and Madeleine Besnard. "Fate of Radiometabolites." In Principles of Radiopharmacology. CRC Press, 2021. http://dx.doi.org/10.1201/9780429288760-9.

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Ichise, Masanori, Yasuyuki Kimura, Hitoshi Shimada, Makoto Higuchi, and Tetsuya Suhara. "PET Quantification in Molecular Brain Imaging Taking into Account the Contribution of the Radiometabolite Entering the Brain." In Perspectives on Nuclear Medicine for Molecular Diagnosis and Integrated Therapy. Springer Japan, 2016. http://dx.doi.org/10.1007/978-4-431-55894-1_17.

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Yano, Yukio. "Effect of Transport on Distribution of Radioions and Radiometabolites." In Biological Transport of Radiotracers. CRC Press, 2020. http://dx.doi.org/10.1201/9780429283062-9.

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