Optimisation of synthesis, purification and reformulation of (R)-[N-Methyl-<sup>11</sup>C]PK11195 for in vivo PET imaging studies

Alves, Vítor H.; Abrunhosa, Antero

doi:10.1109/enbeng.2013.6518428

Cited by 2 publications

(1 citation statement)

References 66 publications

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“…RCYs of 20 ± 6%, with high RCP (over 98%) and moderate molar activity (68.2 ± 18.1 GBq/µmol) at the end of synthesis were obtained (Scheme 9). In 2015, Alves and co-workers suggested an optimised radiolabelling protocol in which the tracer was performed using a captive solvent method, in an HPLC injection loop, with [ 11 C]methyl iodide at room temperature [63]. [64].…”

Section: Microgliamentioning

confidence: 99%

Huntington’s Disease: A Review of the Known PET Imaging Biomarkers and Targeting Radiotracers

et al. 2020

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Huntington’s disease (HD) is a fatal neurodegenerative disease caused by a CAG expansion mutation in the huntingtin gene. As a result, intranuclear inclusions of mutant huntingtin protein are formed, which damage striatal medium spiny neurons (MSNs). A review of Positron Emission Tomography (PET) studies relating to HD was performed, including clinical and preclinical data. PET is a powerful tool for visualisation of the HD pathology by non-invasive imaging of specific radiopharmaceuticals, which provide a detailed molecular snapshot of complex mechanistic pathways within the brain. Nowadays, radiochemists are equipped with an impressive arsenal of radioligands to accurately recognise particular receptors of interest. These include key biomarkers of HD: adenosine, cannabinoid, dopaminergic and glutamateric receptors, microglial activation, phosphodiesterase 10 A and synaptic vesicle proteins. This review aims to provide a radiochemical picture of the recent developments in the field of HD PET, with significant attention devoted to radiosynthetic routes towards the tracers relevant to this disease.

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Section: Microgliamentioning

confidence: 99%

Huntington’s Disease: A Review of the Known PET Imaging Biomarkers and Targeting Radiotracers

et al. 2020

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Use of 55 PET radiotracers under approval of a Radioactive Drug Research Committee (RDRC)

Jackson

Lee

Sowa

et al. 2020

EJNMMI radiopharm. chem.

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Background In the US, EU and elsewhere, basic clinical research studies with positron emission tomography (PET) radiotracers that are generally recognized as safe and effective (GRASE) can often be conducted under institutional approval. For example, in the United States, such research is conducted under the oversight of a Radioactive Drug Research Committee (RDRC) as long as certain requirements are met. Firstly, the research must be for basic science and cannot be intended for immediate therapeutic or diagnostic purposes, or to determine the safety and effectiveness of the PET radiotracer. Secondly, the PET radiotracer must be generally recognized as safe and effective. Specifically, the mass dose to be administered must not cause any clinically detectable pharmacological effect in humans, and the radiation dose to be administered must be the smallest dose practical to perform the study and not exceed regulatory dose limits within a 1-year period. In our experience, the main barrier to using a PET radiotracer under RDRC approval is accessing the required information about mass and radioactive dosing. Results The University of Michigan (UM) has a long history of using PET radiotracers in clinical research studies. Herein we provide dosing information for 55 radiotracers that will enable other PET Centers to use them under the approval of their own RDRC committees. Conclusions The data provided herein will streamline future RDRC approval, and facilitate further basic science investigation of 55 PET radiotracers that target functionally relevant biomarkers in high impact disease states.

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Optimisation of synthesis, purification and reformulation of (R)-[N-Methyl-¹¹C]PK11195 for in vivo PET imaging studies

Cited by 2 publications

References 66 publications

Huntington’s Disease: A Review of the Known PET Imaging Biomarkers and Targeting Radiotracers

Huntington’s Disease: A Review of the Known PET Imaging Biomarkers and Targeting Radiotracers

Use of 55 PET radiotracers under approval of a Radioactive Drug Research Committee (RDRC)

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Optimisation of synthesis, purification and reformulation of (R)-[N-Methyl-11C]PK11195 for in vivo PET imaging studies

Cited by 2 publications

References 66 publications

Huntington’s Disease: A Review of the Known PET Imaging Biomarkers and Targeting Radiotracers

Huntington’s Disease: A Review of the Known PET Imaging Biomarkers and Targeting Radiotracers

Use of 55 PET radiotracers under approval of a Radioactive Drug Research Committee (RDRC)

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Optimisation of synthesis, purification and reformulation of (R)-[N-Methyl-¹¹C]PK11195 for in vivo PET imaging studies