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Journal articles on the topic 'Radiometabolites'

Author: Grafiati

Published: 2 June 2025

Last updated: 31 July 2025

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1

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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2

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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3

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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10

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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11

Shetty, H. Umesha, Sami S. Zoghbi, Jeih-San Liow, et al. "Identification and regional distribution in rat brain of radiometabolites of the dopamine transporter PET radioligand [11C]PE2I." European Journal of Nuclear Medicine and Molecular Imaging 34, no. 5 (2006): 667–78. http://dx.doi.org/10.1007/s00259-006-0277-1.

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12

Volková, Marie, Jana Mandíková, Pavel Bárta, Lucie Navrátilová, Alice Lázníčková, and František Trejtnar. "Thein vivodisposition andin vitrotransmembrane transport of two model radiometabolites of DOTA-conjugated receptor-specific peptides labelled with177Lu." Journal of Labelled Compounds and Radiopharmaceuticals 58, no. 13-14 (2015): 483–89. http://dx.doi.org/10.1002/jlcr.3352.

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13

Ory, Dieter, Andrey Postnov, Michel Koole, et al. "Quantification of TSPO overexpression in a rat model of local neuroinflammation induced by intracerebral injection of LPS by the use of [(18)F]DPA-714 PET." Eur J Nucl Med Mol Imaging 43, no. 1 (2015): 163–72. https://doi.org/10.1007/s00259-015-3172-9.

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PURPOSE: [(18)F]DPA-714 is a radiotracer with high affinity for TSPO. We have characterized the kinetics of [(18)F]DPA-714 in rat brain and evaluated its ability to quantify TSPO expression with PET using a neuroinflammation model induced by unilateral intracerebral injection of lipopolysaccharide (LPS). METHODS: Dynamic small-animal PET scans with [(18)F]DPA-714 were performed in Wistar rats on a FOCUS-220 system for up to 3 h. Both plasma and perfused brain homogenates were analysed using HPLC to quantify radiometabolites. Full kinetic modelling of [(18)F]DPA-714 brain uptake was perfor

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14

Finnema, Sjoerd J., B. Bang-Andersen, M. Jørgensen, et al. "COMT inhibition prevents the formation of lipophilic radiometabolites of catechols, — An example with (S)-[11C]N-methyl-NNC 01-0259." NeuroImage 41 (January 2008): T91. http://dx.doi.org/10.1016/j.neuroimage.2008.04.060.

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15

Zheng, Chao, Daniel Holden, Ming-Qiang Zheng, et al. "A metabolically stable PET tracer for imaging synaptic vesicle protein 2A: synthesis and preclinical characterization of [18F]SDM-16." European Journal of Nuclear Medicine and Molecular Imaging 49, no. 5 (2021): 1482–96. http://dx.doi.org/10.1007/s00259-021-05597-5.

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Abstract Purpose To quantify the synaptic vesicle glycoprotein 2A (SV2A) changes in the whole central nervous system (CNS) under pathophysiological conditions, a high affinity SV2A PET radiotracer with improved in vivo stability is desirable to minimize the potential confounding effect of radiometabolites. The aim of this study was to develop such a PET tracer based on the molecular scaffold of UCB-A, and evaluate its pharmacokinetics, in vivo stability, specific binding, and nonspecific binding signals in nonhuman primate brains, in comparison with [11C]UCB-A, [11C]UCB-J, and [18F]SynVesT-1.

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Malherbe, Cécile, Rudy Bidault, Claude Netter, Denis Guilloteau, Johnny Vercouillie, and Nicolas Arlicot. "Development of a Fast and Facile Analytical Approach to Quantify Radiometabolites in Human Plasma Samples Using Ultra High Performance Liquid Chromatography." American Journal of Analytical Chemistry 10, no. 05 (2019): 185–201. http://dx.doi.org/10.4236/ajac.2019.105016.

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17

Bertoglio, Daniele, Jeroen Verhaeghe, Alan Miranda, et al. "Longitudinal preclinical evaluation of the novel radioligand [11C]CHDI-626 for PET imaging of mutant huntingtin aggregates in Huntington’s disease." European Journal of Nuclear Medicine and Molecular Imaging 49, no. 4 (2021): 1166–75. http://dx.doi.org/10.1007/s00259-021-05578-8.

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Abstract Purpose As several therapies aimed at lowering mutant huntingtin (mHTT) brain levels in Huntington’s disease (HD) are currently being investigated, noninvasive positron emission tomography (PET) imaging of mHTT could be utilized to directly evaluate therapeutic efficacy and monitor disease progression. Here we characterized and longitudinally assessed the novel radioligand [11C]CHDI-626 for mHTT PET imaging in the zQ175DN mouse model of HD. Methods After evaluating radiometabolites and radioligand kinetics, we conducted longitudinal dynamic PET imaging at 3, 6, 9, and 13 months of age

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Kobayashi, Masato, Teresa Jiang, Sanjay Telu, et al. "11C-DPA-713 has much greater specific binding to translocator protein 18 kDa (TSPO) in human brain than 11C-(R)-PK11195." Journal of Cerebral Blood Flow & Metabolism 38, no. 3 (2017): 393–403. http://dx.doi.org/10.1177/0271678x17699223.

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Positron emission tomography (PET) radioligands for translocator protein 18 kDa (TSPO) are widely used to measure neuroinflammation, but controversy exists whether second-generation radioligands are superior to the prototypical agent 11C-( R)-PK11195 in human imaging. This study sought to quantitatively measure the “signal to background” ratio (assessed as binding potential ( BPND)) of 11C-( R)-PK11195 compared to one of the most promising second-generation radioligands, 11C-DPA-713. Healthy subjects had dynamic PET scans and arterial blood measurements of radioligand after injection of either

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19

Finnema, Sjoerd J., Nabeel B. Nabulsi, Joël Mercier, et al. "Kinetic evaluation and test–retest reproducibility of [11C]UCB-J, a novel radioligand for positron emission tomography imaging of synaptic vesicle glycoprotein 2A in humans." Journal of Cerebral Blood Flow & Metabolism 38, no. 11 (2017): 2041–52. http://dx.doi.org/10.1177/0271678x17724947.

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Synaptic vesicle glycoprotein 2A (SV2A) is ubiquitously present in presynaptic terminals. Here we report kinetic modeling and test–retest reproducibility assessment of the SV2A positron emission tomography (PET) radioligand [11C]UCB-J in humans. Five volunteers were examined twice on the HRRT after bolus injection of [11C]UCB-J. Arterial blood samples were collected for measurements of radiometabolites and free fraction. Regional time–activity curves were analyzed with 1-tissue (1T) and 2-tissue (2T) compartment models to estimate volumes of distribution ( VT). Parametric maps were generated u

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20

Ludwig, Friedrich-Alexander, Steffen Fischer, René Smits, et al. "Exploring the Metabolism of (+)-[18F]Flubatine In Vitro and In Vivo: LC-MS/MS Aided Identification of Radiometabolites in a Clinical PET Study †." Molecules 23, no. 2 (2018): 464. http://dx.doi.org/10.3390/molecules23020464.

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21

Peyronneau, Marie-Anne, Wadad Saba, Sébastien Goutal, et al. "[18F]Fallypride: Metabolism studies and quantification of the radiotracer and its radiometabolites in plasma using a simple and rapid solid-phase extraction method." Nuclear Medicine and Biology 40, no. 7 (2013): 887–95. http://dx.doi.org/10.1016/j.nucmedbio.2013.06.003.

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22

Hörmann, Anton Amadeus, Maximilian Klingler, Maliheh Rezaeianpour, et al. "Initial In Vitro and In Vivo Evaluation of a Novel CCK2R Targeting Peptide Analog Labeled with Lutetium-177." Molecules 25, no. 19 (2020): 4585. http://dx.doi.org/10.3390/molecules25194585.

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Targeting of cholecystokinin-2 receptor (CCK2R) expressing tumors using radiolabeled minigastrin (MG) analogs is hampered by rapid digestion of the linear peptide in vivo. In this study, a new MG analog stabilized against enzymatic degradation was investigated in preclinical studies to characterize the metabolites formed in vivo. The new MG analog DOTA-DGlu-Pro-Tyr-Gly-Trp-(N-Me)Nle-Asp-1Nal-NH2 comprising site-specific amino acid substitutions in position 2, 6 and 8 and different possible metabolites thereof were synthesized. The receptor interaction of the peptide and selected metabolites wa

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Auvity, Sylvain, Hélène Chapy, Sébastien Goutal, et al. "Diphenhydramine as a selective probe to study H+-antiporter function at the blood–brain barrier: Application to [11C]diphenhydramine positron emission tomography imaging." Journal of Cerebral Blood Flow & Metabolism 37, no. 6 (2016): 2185–95. http://dx.doi.org/10.1177/0271678x16662042.

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Diphenhydramine, a sedative histamine H1-receptor (H1R) antagonist, was evaluated as a probe to measure drug/H+-antiporter function at the blood–brain barrier. In situ brain perfusion experiments in mice and rats showed that diphenhydramine transport at the blood–brain barrier was saturable, following Michaelis–Menten kinetics with a Km = 2.99 mM and Vmax = 179.5 nmol s−1 g−1. In the pharmacological plasma concentration range the carrier-mediated component accounted for 77% of diphenhydramine influx while passive diffusion accounted for only 23%. [14C]Diphenhydramine blood–brain barrier transp

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Tolmachev, Vladimir, Cheng-Bin Yim, Johan Rajander, et al. "Comparative Evaluation of Anti-HER2 Affibody Molecules Labeled with 64Cu Using NOTA and NODAGA." Contrast Media & Molecular Imaging 2017 (2017): 1–12. http://dx.doi.org/10.1155/2017/8565802.

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Imaging using affibody molecules enables discrimination between breast cancer metastases with high and low expression of HER2, making appropriate therapy selection possible. This study aimed to evaluate if the longer half-life of 64Cu (T1/2 = 12.7 h) would make 64Cu a superior nuclide compared to 68Ga for PET imaging of HER2 expression using affibody molecules. The synthetic ZHER2:S1 affibody molecule was conjugated with the chelators NOTA or NODAGA and labeled with 64Cu. The tumor-targeting properties of 64Cu-NOTA-ZHER2:S1 and 64Cu-NODAGA-ZHER2:S1 were evaluated and compared with the targetin

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Lu, Shuiyu, Mohammad B. Haskali, Kevin M. Ruley та ін. "PET ligands [18F]LSN3316612 and [11C]LSN3316612 quantify O-linked-β-N-acetyl-glucosamine hydrolase in the brain". Science Translational Medicine 12, № 543 (2020): eaau2939. http://dx.doi.org/10.1126/scitranslmed.aau2939.

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We aimed to develop effective radioligands for quantifying brain O-linked-β-N-acetyl-glucosamine (O-GlcNAc) hydrolase (OGA) using positron emission tomography in living subjects as tools for evaluating drug target engagement. Posttranslational modifications of tau, a biomarker of Alzheimer’s disease, by O-GlcNAc through the enzyme pair OGA and O-GlcNAc transferase (OGT) are inversely related to the amounts of its insoluble hyperphosphorylated form. Increase in tau O-GlcNAcylation by OGA inhibition is believed to reduce tau aggregation. LSN3316612, a highly selective and potent OGA ligand [half

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Vorobyeva, Schulga, Rinne, et al. "Indirect Radioiodination of DARPin G3 Using N-succinimidyl-Para-Iodobenzoate Improves the Contrast of HER2 Molecular Imaging." International Journal of Molecular Sciences 20, no. 12 (2019): 3047. http://dx.doi.org/10.3390/ijms20123047.

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Radionuclide molecular imaging of human epidermal growth factor receptor 2 (HER2) in breast and gastroesophageal cancer might be used to stratify patients for HER2-targeted therapy as well as monitor treatment response and disease progression. Designed ankyrin repeat proteins (DARPins) are small engineered scaffold proteins with favorable properties for molecular imaging. Herein we compared two methods for labeling the anti-HER2 DARPin (HE)3-G3, direct and indirect radioiodination. We hypothesized that the use of N-succinimidyl-para-iodobenzoate (SPIB) for radioiodination would facilitate the

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Egfjord, M., and K. Olgaard. "Aldosterone metabolism in the isolated perfused liver of R and S hypertension-prone Dahl rats." American Journal of Physiology-Endocrinology and Metabolism 262, no. 4 (1992): E488—E496. http://dx.doi.org/10.1152/ajpendo.1992.262.4.e488.

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The effect of a chronic oral salt load on hepatic metabolism of aldosterone was examined in isolated livers of salt-resistant (R) and salt-sensitive (S) hypertension-prone male Dahl rats perfused with d-[4-14C]aldosterone (10(-9) M). Aldosterone was analyzed by radioimmunoassay and [4-14C]aldosterone radiometabolites by high-performance liquid chromatography. In salt-loaded S rats, systolic blood pressure was 30 mmHg higher than in the other three groups (P less than 0.01). In S rats, on standard and high-salt diets, plasma renin activity was 64% (P less than 0.001) and 50% (P less than 0.01)

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Carpinelli, Assunta, Paolo Rainone, Sara Belloli, et al. "Radiosynthesis and Preclinical Evaluation of 11C-VA426, a Cyclooxygenase-2 Selective Ligand." Contrast Media & Molecular Imaging 2019 (September 24, 2019): 1–12. http://dx.doi.org/10.1155/2019/5823261.

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Cyclooxygenase-2 (COX-2) is involved in the inflammatory response, and its recurrent overexpression in cancers as well as in neurodegenerative disorders has made it an important target for therapy. For this reason, noninvasive imaging of COX-2 expression may represent an important diagnostic tool. In this work, a COX-2 inhibitor analogue, VA426 [1-(4-fluorophenyl)-3-(2-methoxyethyl)-2-methyl-5-(4-(methylsulfonil)phenyl)-1H-pyrrole], was synthesized and radiolabelled with the 11C radioisotope. The ex vivo biodistribution profile of 11C-VA426 was evaluated in the brain and periphery of healthy r

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Amini, Nahid, Ryuji Nakao, Magnus Schou, and Christer Halldin. "Identification of PET radiometabolites by cytochrome P450, UHPLC/Q-ToF-MS and fast radio-LC: applied to the PET radioligands [11C]flumazenil, [18F]FE-PE2I, and [11C]PBR28." Analytical and Bioanalytical Chemistry 405, no. 4 (2012): 1303–10. http://dx.doi.org/10.1007/s00216-012-6541-2.

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Ludwig, Friedrich-Alexander, Erik Laurini, Judith Schmidt, Sabrina Pricl, Winnie Deuther-Conrad та Bernhard Wünsch. "[18F]Fluspidine—A PET Tracer for Imaging of σ1 Receptors in the Central Nervous System". Pharmaceuticals 17, № 2 (2024): 166. http://dx.doi.org/10.3390/ph17020166.

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σ1 receptors play a crucial role in various neurological and neurodegenerative diseases including pain, psychosis, Alzheimer’s disease, and depression. Spirocyclic piperidines represent a promising class of potent σ1 receptor ligands. The relationship between structural modifications and σ1 receptor affinity and selectivity over σ2 receptors led to the 2-fluoroethyl derivative fluspidine (2, Ki = 0.59 nM). Enantiomerically pure (S)-configured fluspidine ((S)-2) was prepared by the enantioselective reduction of the α,β-unsaturated ester 23 with NaBH4 and the enantiomerically pure co-catalyst (S

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Nag, S., L. Lehmann, G. Kettschau, et al. "Development of a novel fluorine-18 labeled deuterated fluororasagiline ([18F]fluororasagiline-D2) radioligand for PET studies of monoamino oxidase B (MAO-B)." Bioorg Med Chem. 21, no. 21 (2013): 6634–41. https://doi.org/10.1016/j.bmc.2013.08.019.

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The objective of this study was to synthesize and evaluate a novel fluorine-18 labeled deuterium substituted analogue of rasagiline (9, [18F]fluororasagiline-D2) as a potential PET radioligand for studies of monoamine oxidase B (MAO-B). The precursor compound (6) and reference standard (7) were synthesized in multi-step syntheses. Radiolabeling of 9 was accomplished by a two-step synthesis, compromising a nucleophilic substitution followed by hydrolysis of the sulfamidate group. The incorporation radiochemical yield from fluorine-18 fluoride was higher than 30%, the radiochemical purity was &g

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Vicidomini, Caterina, Mariarosaria Panico, Adelaide Greco, et al. "In vivo imaging and characterization of [(18)F]DPA-714, a potential new TSPO ligand, in mouse brain and peripheral tissues using small-animal PET." Nucl Med Biol. 42, no. 3 (2014): 309–16. https://doi.org/10.1016/j.nucmedbio.2014.11.009.

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INTRODUCTION: The translocator protein 18kDa (TSPO), a biochemical marker of neuroinflammation, is highly expressed in the brain activated microglia and it is also expressed by peripheral inflammatory cells and normal peripheral tissues. Thus, development of radioligands for the TSPO may contribute to further understanding the in vivo TSPO function in central and peripheral inflammatory processes and other pathologies. Here, we report the biodistribution, the specific binding and the radiometabolites of [(18)F]DPA-714, a promising fluorinated PET radiotracer, in normal mice using a microP

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Hashimoto, Hiroki, Kazunori Kawamura, Makoto Takei, et al. "Identification of a major radiometabolite of [ 11 C]PBB3." Nuclear Medicine and Biology 42, no. 12 (2015): 905–10. http://dx.doi.org/10.1016/j.nucmedbio.2015.08.006.

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Keller, Thomas, Anna Krzyczmonik, Sarita Forsback, et al. "Radiosynthesis and Preclinical Evaluation of [18F]F-DPA, A Novel Pyrazolo[1,5a]pyrimidine Acetamide TSPO Radioligand, in Healthy Sprague Dawley Rats." Molecular Imaging & Biology 19, no. 5 (2017): 736–45. https://doi.org/10.1007/s11307-016-1040-z.

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PURPOSE: Many neurological conditions result in the overexpression of the translocator protein 18 kDa (TSPO), today recognized as a biomarker for microglial activation and neuroinflammation imaging. The pyrazolo[1,5-a]pyrimidine acetamides are a particularly attractive class of TSPO-specific ligands, prompting the development of several positron emission tomography (PET) radiotracers. This includes F-DPA, a recently reported fluorinated ligand (K <sub>i</sub> =&thinsp;1.7 nM), wherein the fluorine atom is directly linked to the phenyl moiety without the presence of an alky

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Gourand, F., P. Emond, J. P. Bergström, et al. "A radiometabolite study of the serotonin transporter PET radioligand [11C]MADAM." Nuclear Medicine and Biology 41, no. 6 (2014): 501–6. http://dx.doi.org/10.1016/j.nucmedbio.2014.03.022.

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36

Lohith, Talakad G., Tetsuya Tsujikawa, Fabrice G. Siméon, et al. "Comparison of two PET radioligands, [11C]FPEB and [11C]SP203, for quantification of metabotropic glutamate receptor 5 in human brain." Journal of Cerebral Blood Flow & Metabolism 37, no. 7 (2016): 2458–70. http://dx.doi.org/10.1177/0271678x16668891.

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Of the two 18F-labeled PET ligands currently available to image metabotropic glutamate receptor 5 (mGluR5), [18F]FPEB is reportedly superior because [18F]SP203 undergoes glutathionlyation, generating [18F]-fluoride ion that accumulates in brain and skull. To allow multiple PET studies on the same day with lower radiation exposure, we prepared [11C]FPEB and [11C]SP203 from [11C]hydrogen cyanide and compared their abilities to accurately quantify mGluR5 in human brain, especially as regards radiometabolite accumulation. Genomic plot was used to estimate the ratio of specific-to-nondisplaceable u

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Vasdev, Neil, and Thomas Collier. "Design and Prototype of an Automated Column-Switching HPLC System for Radiometabolite Analysis." Pharmaceuticals 9, no. 3 (2016): 51. http://dx.doi.org/10.3390/ph9030051.

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Moein, Mohammad Mahdi, Miklós Tóth, Lenke Tari, Andrea Varrone, Mohamed Abdel-Rehim, and Christer Halldin. "New approach in radiometabolite analysis of positron emission tomography (PET) radioligands; lead-shielded microextraction by packed sorbent as a tool for in vivo radiometabolite analysis of [11C]SMW139 in rat plasma." Talanta 208 (February 2020): 120449. http://dx.doi.org/10.1016/j.talanta.2019.120449.

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McMahon, Adam W., N. S. Pelton, E. C. Barnett, G. Brown, and P. J. Tyrrell. "The use of restricted access solid phase extraction for [11C](R)-PK11195 radiometabolite measurements." NeuroImage 41 (January 2008): T95. http://dx.doi.org/10.1016/j.neuroimage.2008.04.064.

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Zoghbi, S. S., J. S. Liow, F. Yasuno, et al. "11C-Loperamide and Its N-Desmethyl Radiometabolite Are Avid Substrates for Brain Permeability-Glycoprotein Efflux." Journal of Nuclear Medicine 49, no. 4 (2008): 649–56. http://dx.doi.org/10.2967/jnumed.107.047308.

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Nakao, Ryuji, and Christer Halldin. "A simplified radiometabolite analysis procedure for PET radioligands using a solid phase extraction with micellar medium." Nuclear Medicine and Biology 40, no. 5 (2013): 658–63. http://dx.doi.org/10.1016/j.nucmedbio.2013.02.007.

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Moein, Mohammad Mahdi, Ryuji Nakao, Nahid Amini, Mohamed Abdel-Rehim, Magnus Schou, and Christer Halldin. "Sample preparation techniques for radiometabolite analysis of positron emission tomography radioligands; trends, progress, limitations and future prospects." TrAC Trends in Analytical Chemistry 110 (January 2019): 1–7. http://dx.doi.org/10.1016/j.trac.2018.10.019.

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Pamie-George, Matilah, Meijuan Jiang, Shiyu Tang, et al. "190. Robust Quantification of Phosphodiesterase-4D Using Carbon-11 Pet Radioligands in Monkey Brain Without Radiometabolite Contamination." Biological Psychiatry 95, no. 10 (2024): S177. http://dx.doi.org/10.1016/j.biopsych.2024.02.425.

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Qiu, Lin, Hao Jiang, Kevin Cho, et al. "Radiometabolite structural confirmation of [11C]CS1P1, a promising radiotracer for imaging neuroinflammation of patients with Multiple Sclerosis." Nuclear Medicine and Biology 126-127 (November 2023): 108542. http://dx.doi.org/10.1016/j.nucmedbio.2023.108542.

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Nakao, Ryuji, and Christer Halldin. "“Mixed” anionic and non-ionic micellar liquid chromatography for high-speed radiometabolite analysis of positron emission tomography radioligands." Journal of Chromatography A 1281 (March 2013): 54–59. http://dx.doi.org/10.1016/j.chroma.2013.01.071.

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Zhang, Xiang-Yang, Fumihiko Yasuno, Sami S. Zoghbi, et al. "Quantification of serotonin 5-HT1A receptors in humans with [11C](R)-(−)-RWAY: Radiometabolite(s) likely confound brain measurements." Synapse 61, no. 7 (2007): 469–77. http://dx.doi.org/10.1002/syn.20392.

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Schröder, Susann, Thu Hang Lai, Magali Toussaint, et al. "PET Imaging of the Adenosine A2A Receptor in the Rotenone-Based Mouse Model of Parkinson’s Disease with [18F]FESCH Synthesized by a Simplified Two-Step One-Pot Radiolabeling Strategy." Molecules 25, no. 7 (2020): 1633. http://dx.doi.org/10.3390/molecules25071633.

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The adenosine A2A receptor (A2AR) is regarded as a particularly appropriate target for non-dopaminergic treatment of Parkinson’s disease (PD). An increased A2AR availability has been found in the human striatum at early stages of PD and in patients with PD and dyskinesias. The aim of this small animal positron emission tomography/magnetic resonance (PET/MR) imaging study was to investigate whether rotenone-treated mice reflect the aspect of striatal A2AR upregulation in PD. For that purpose, we selected the known A2AR-specific radiotracer [18F]FESCH and developed a simplified two-step one-pot

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Lau, Joseph, Hwan Lee, Julie Rousseau, François Bénard, and Kuo-Shyan Lin. "Application of Cleavable Linkers to Improve Therapeutic Index of Radioligand Therapies." Molecules 27, no. 15 (2022): 4959. http://dx.doi.org/10.3390/molecules27154959.

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Radioligand therapy (RLT) is an emergent drug class for cancer treatment. The dose administered to cancer patients is constrained by the radiation exposure to normal tissues to maintain an appropriate therapeutic index. When a radiopharmaceutical or its radiometabolite is retained in the kidneys, radiation dose deposition in the kidneys can become a dose-limiting factor. A good exemplar is [177Lu]Lu-DOTATATE, where patients receive a co-infusion of basic amino acids for nephroprotection. Besides peptides, there are other classes of targeting vectors like antibody fragments, antibody mimetics,

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Nag, Sangram, Prodip Datta, Anton Forsberg Morén, et al. "Labeling of Bruton’s Tyrosine Kinase (BTK) Inhibitor [11C]BIO-2008846 in Three Different Positions and Measurement in NHP Using PET." International Journal of Molecular Sciences 25, no. 14 (2024): 7870. http://dx.doi.org/10.3390/ijms25147870.

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Bruton’s tyrosine kinase (BTK) is pivotal in B-cell signaling and a target for potential anti-cancer and immunological disorder therapies. Improved selective reversible BTK inhibitors are in demand due to the absence of direct BTK engagement measurement tools. Promisingly, PET imaging can non-invasively evaluate BTK expression. In this study, radiolabeled BIO-2008846 ([11C]BIO-2008846-A), a BTK inhibitor, was used for PET imaging in NHPs to track brain biodistribution. Radiolabeling BIO-2008846 with carbon-11, alongside four PET scans on two NHPs each, showed a homogeneous distribution of [11C

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Hattori, Yasushi, Chie Seki, Jun Maeda, et al. "Quantification of monoacylglycerol lipase and its occupancy by an exogenous ligand in rhesus monkey brains using [¹⁸F]T-401 and PET." Journal of Cerebral Blood Flow & Metabolism 42, no. 4 (2021): 656–66. http://dx.doi.org/10.1177/0271678x211058285.

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Monoacylglycerol lipase (MAGL) is a cytosolic serine hydrolase that cleaves monoacylglycerols into fatty acids and is a potential target for the novel treatment of CNS disorders related to the endocannabinoid system and neuroinflammation. We have developed [18F]T-401 as a selective Positron emission tomography (PET) imaging agent for MAGL. In this study, we determined an analytical method to quantify MAGL availability and its occupancy by an exogenous inhibitor in rhesus monkey brains using [18F]T-401-PET. In rhesus monkeys, regional time-activity curves were described well when using an exten

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