Efficient <i>in‐loop</i> synthesis of high specific radioactivity [<sup>11</sup>C]carfentanil

Studenov, Andrei R.; Jivan, Salma; Buckley, K.; Adam, Michael J.

doi:10.1002/jlcr.722

Cited by 16 publications

(13 citation statements)

References 12 publications

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“…Radiochemistry production facilities typically synthesize [ 11 C]CFN by methylation of the carboxylate precursor. In early syntheses, this was accomplished using [ 11 C]MeI and the resulting [ 11 C]CFN could be purified using semipreparative HPLC or solid‐phase extraction (SPE) . More recently, groups often methylate the precursor using [ 11 C]MeOTf instead and purify by SPE according to the method developed by Jewett .…”

Section: Introductionmentioning

confidence: 99%

An updated synthesis of [¹¹C]carfentanil for positron emission tomography (PET) imaging of the μ‐opioid receptor

Blecha

Henderson

Hockley

et al. 2017

Labelled Comp Radiopharmac

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[ C]Carfentanil ([ C]CFN) is a selective radiotracer for in vivo positron emission tomography imaging studies of the μ-opioid system that, in our laboratories, is synthesized by methylation of the corresponding carboxylate precursor with [ C]MeOTf, and purified using a C2 solid-phase extraction cartridge. Changes in the commercial availability of common C2 cartridges have necessitated future proofing the synthesis of [ C]CFN to maintain reliable delivery of the radiotracer for clinical imaging studies. An updated synthesis of [ C]CFN is reported that replaces a now obsolete purification cartridge with a new commercially available version and also substitutes the organic solvents used in traditional production methods with ethanol.

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Section: Introductionmentioning

confidence: 99%

An updated synthesis of [¹¹C]carfentanil for positron emission tomography (PET) imaging of the μ‐opioid receptor

Blecha

Henderson

Hockley

et al. 2017

Labelled Comp Radiopharmac

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“…Using these methods, a number of human PET papers have been published, including the first‐in‐man paper by Frost et al . For a summary of other [ 11 C]carfentanil PET publications, readers are directed to recent reviews …”

Section: μ‐Selective Radiotracersmentioning

confidence: 99%

Positron emission tomography radioligands for the opioid system

Dannals

2013

Labelled Comp Radiopharmac

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Opiate receptors are found in the brain, the spinal cord, some peripheral sensory neurons, and the gastrointestinal tract. Naturally occurring and synthetic opiate ligands exert their influence on a wide variety of processes including analgesia, euphoria, dysphoria, sedation, respiratory depression, and miosis and are frequently topics for discussions on addiction and physical dependence. This review looks at the history of positron emission tomography radioligands for probing this receptor system.

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“…Indeed, insulin secretion is regulated by the membrane potential of the -cell, which depends on the activity of ATP-sensitive K + channels (K ATP channels) in the plasma membrane. A decay corrected yield, with respect to [ 11 C]CH 3 I, of [ 11 C]carfentanil was 64 % with the synthesis time of 21 min [96]. The second one is the efficient in-loop synthesis of high specific radioactivity [ 11 C]carfentanil [95], a μ-opioid agonist (Fig.…”

Section: Miscellaneous Types Of Receptor Ligandsmentioning

confidence: 99%

State of Art in 11C Labelled Radiotracers Synthesis

Allard

Fouquet

James

et al. 2008

CMC

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Positron Emission Tomography has become a powerful scientific and clinical tool probing biochemical processes in the human body. Their clinical applications have proven to be vital in the evaluation and diagnosis of diseases. This is due, in large part, to advances in instrumentation and synthetic chemistry. Carbon-11 is a valuable radionuclide in PET as it virtually permits the synthesis of radiolabelled versions of any compound of interest. The syntheses with carbon-11 present several features: limited number of labelled precursors, sub-micromolar amounts of the starting materials, and a need for the introduction of the radioisotope as late as possible in the synthesis. All of these reasons have restricted complex radiosyntheses. The short half-life of carbon-11 (20.4 min) requires the rapid preparation and purification of carbon-11 labelled molecules. Those have to be carried out immediately before use from cyclotron produced precursors ([11C]CO2, [11C]CO, [11C]CH4) or reagents rapidly prepared from them ([11C]CH3I, [11C]COCl2, [11C]HCN). As a consequence carbon-11 has been underused compared to fluorine-18. However, because of the increasing molecular complexity and diversity of biologically active compounds, there is a need for new methodologies giving access in short time and high yield to radioactive (11)C-probes. The aim of this review is to emphasize the methodologies used in this field and to give a comprehensive overview of the numerous advances, which occurred over the past decade. In addition, for each labelling technique or reaction reported, a special attention has been brought to classify the applications in function of the targeted medical domain.

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Efficient in‐loop synthesis of high specific radioactivity [¹¹C]carfentanil

Abstract: Summary

Cited by 16 publications

References 12 publications

An updated synthesis of [¹¹C]carfentanil for positron emission tomography (PET) imaging of the μ‐opioid receptor

An updated synthesis of [¹¹C]carfentanil for positron emission tomography (PET) imaging of the μ‐opioid receptor

Positron emission tomography radioligands for the opioid system

State of Art in 11C Labelled Radiotracers Synthesis

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Efficient in‐loop synthesis of high specific radioactivity [11C]carfentanil

Abstract: Summary

Cited by 16 publications

References 12 publications

An updated synthesis of [11C]carfentanil for positron emission tomography (PET) imaging of the μ‐opioid receptor

An updated synthesis of [11C]carfentanil for positron emission tomography (PET) imaging of the μ‐opioid receptor

Positron emission tomography radioligands for the opioid system

State of Art in 11C Labelled Radiotracers Synthesis

Contact Info

Product

Resources

About

Efficient in‐loop synthesis of high specific radioactivity [¹¹C]carfentanil

An updated synthesis of [¹¹C]carfentanil for positron emission tomography (PET) imaging of the μ‐opioid receptor

An updated synthesis of [¹¹C]carfentanil for positron emission tomography (PET) imaging of the μ‐opioid receptor