Improved syntheses of the PET radioligands, [11C]FLB 457, [11C]MDL 100907 and [11C]β‐CIT‐FE, by the use of [11C]methyl triflate

doi:10.1002/(SICI)1099-1344(199806)41:6<545::AID-JLCR99>3.0.CO;2-7

Paper

Improved syntheses of the PET radioligands, [11C]FLB 457, [11C]MDL 100907 and [11C]β‐CIT‐FE, by the use of [11C]methyl triflate

Published Jun 1, 1998 · C. Lundkvist, J. Sandell, K. Någren

Journal of Labelled Compounds and Radiopharmaceuticals

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Abstract

The highly reactive labelling agent, [11C]methyl triflate, was used to synthesise three recently developed PET radioligands. The labelling reactions were 11C-methylations of phenols for the preparations of the D2 receptor radioligand, [11C]FLB 457, and the 5-HT2A receptor radioligand, [11C]MDL 100907, and 11C-methylation of a carboxylic acid for the preparation of the dopamine transporter radioligand, [11C]β-CIT-FE. The synthesis of the 5-HT1A receptor radioligand, [O-methyl-11C]WAY-100635, was used to establish general reaction conditions for the methylation of phenols with [11C]methyl triflate. Compared to the previous use of [11C]methyl iodide in these radiosyntheses, [11C]methyl triflate demanded less precursor, allowed faster reactions and improved radiochemical yields. Normal-phase HPLC was used to speed up product purifications (except for [11C]β-CIT-FE). Hence, preparation times were shorter, resulting in radioligands with higher specific radioactivity. © 1998 John Wiley & Sons, Ltd.

Study Snapshot

[11C]methyl triflate improves the synthesis of PET radioligands, requiring less precursor, faster reactions, and higher radiochemical yields compared to previous methods.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Improved syntheses of the PET radioligands, [11C]FLB 457, [11C]MDL 100907 and [11C]β‐CIT‐FE, by the use of [11C]methyl triflate

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References

[125I]β-CIT-FE and [125I]β-CIT-FP are superior to [125I]β-CIT for dopamine transporter visualization: Autoradiographic evaluation in the human brain

[125I]-CIT-FE and -CIT-FP are more specific than -CIT for in vivo studies of dopamine transporters in the human brain.

Autoradiographic localization of 5-HT1A receptors in the post-mortem human brain using [3H]WAY-100635 and [11C]WAY-100635

[3H]WAY-100635 selectively labels 5-HT1A receptors in the human brain, providing detailed information on their distribution and potential for in vivo studies.

Improved synthesis of β-CIT and [11C]β-CIT labeled at nitrogen or oxygen positions

This study improved the synthesis of -CIT and [11C]-CIT, enabling efficient separation of nitrogen and oxygen-labeled radiotracer precursors.

Synthesis of unlabelled, 3H‐ and 125I‐labelled β‐CIT and its ϖ‐fluoroalkyl analogues β‐CIT‐FE and β‐CIT‐FP, including synthesis of precursors

This study demonstrates the successful synthesis of -CIT and its fluoroalkyl analogues, -CIT-FE and -CIT-FP, for use in autoradiographic examination of human brain sections.

Exquisite delineation of 5-HT1A receptors in human brain with PET and [carbonyl-11 C]WAY-100635.

[carbonyl-11 C]WAY-100635 is a superior radioligand for PET studies of 5-HT1A receptors in human brain, providing exquisite delineation of receptor-rich regions.

Citations

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Radiotracers for imaging of Parkinson's disease.

SPECT and PET imaging radiotracers have advanced our understanding of Parkinson's disease, aiding in diagnosis and monitoring disease progression.

Dopaminergic and serotonergic mechanisms in the modulation of pain: In vivo studies in human brain

Dopamine acting on striatal dopamine D 2 /D 3 receptors and serotonin acting on cortical 5-HT 1A and 5-HT 2A receptors contribute to top-down pain regulation in humans.

Development of "[11C]kits" for a fast, efficient and reliable production of carbon-11 labeled radiopharmaceuticals for Positron Emission Tomography.

"[11C]kits" enable fast, efficient, and reliable production of carbon-11 radiotracers for Positron Emission Tomography, overcoming technical challenges.

High-Affinity Dopamine D2/D3 PET Radioligands 18F-Fallypride and 11C-FLB457: A Comparison of Kinetics in Extrastriatal Regions Using a Multiple-Injection Protocol

11C-FLB457 is more sensitive to subtle changes in low-receptor-density cortical regions than 18F-fallypride, while both radioligands can image extrastriatal D2/D3 receptors.

Challenges for Developing PET Tracers: Isotopes, Chemistry, and Regulatory Aspects.

Advances in PET radiochemistry and regulatory requirements are expected to increase the number of radiotracers transitioning from clinical research to clinical studies, benefiting central nervous system research.

[(11)C]PR04.MZ, a promising DAT ligand for low concentration imaging: Synthesis, efficient (11)C-O-methylation and initial small animal PET studies.

[(11)C]PR04.MZ, a highly selective dopamine transporter inhibitor, shows potential as a PET radioligand for non-invasive exploration of striatal and extrastriatal DAT populations in the brain.

Age-related loss of olfactory sensitivity: Association to dopamine transporter binding in putamen

Age-related olfactory deficits are linked to reduced dopamine transporter binding in the putamen, which also affects odor sensitivity independently of age.