Studies to label alfentanil with carbon-11

Feliu, Anthony L.

doi:10.1016/0883-2889(92)90061-i

Cited by 3 publications

(2 citation statements)

References 15 publications

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“…4), including [ 11 C]alfentanil [92], [ 11 C]-ohmefentanil [93], [ 18 F]fluorofentanil [94] and the 4,5-epoxymorphinan, [ 11 C]etorphine [95]. Hydromorphone (Dilaudid ® ), a weaker full µ-agonist, has been labeled with carbon-11 [96].…”

Section: Radioligands For Pet [ 11 C]carfentanil and Other µ-Opioid Rmentioning

confidence: 99%

PET and SPECT Imaging of the Opioid System: Receptors, Radioligands and Avenues for Drug Discovery and Development

Lever¹

2007

CPD

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As we celebrate the bicentennial of the isolation of morphine by Sertürner, opioids continue to dominate major sectors of the analgesic market worldwide. The pharmaceutical industry stands to benefit greatly from molecular imaging in preclinical and early clinical trials of new or improved opioid drugs. At this juncture, it seems fitting to summarize the past twenty or so years of research on molecular imaging of the opioid system from the viewpoint of drug discovery and development. Opioid receptors were first imaged in human volunteers by positron emission tomography (PET) in 1984. Now, quantitative PET imaging of the major opioid receptor types (micro, delta , kappa) is possible in the brain and peripheral organs of healthy persons and patient populations. Radioligands are under development for single photon emission computed tomography (SPECT) of opioid receptors as well. These functional, nuclear imaging techniques can trace the fate of radiolabeled molecules directly, but non-invasively, and allow precise pharmacokinetic and pharmacodynamic measurements. Molecular imaging provides unique data that can aid in selecting the best drug candidates, determining optimal dosing regimens, clearing regulatory hurdles and lowering risks of failure. Using a historical perspective, this review touches on opioid receptors as drug targets, and focuses on the status and use of radiotracers for opioid receptor PET and SPECT. Selected studies are discussed to illustrate the power of molecular imaging for facilitating opioid drug discovery and development.

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Section: Radioligands For Pet [ 11 C]carfentanil and Other µ-Opioid Rmentioning

confidence: 99%

PET and SPECT Imaging of the Opioid System: Receptors, Radioligands and Avenues for Drug Discovery and Development

Lever¹

2007

CPD

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“…In 1992, a collaborative effort produced [ 11 C]ohmefentanyl at moderate specific activity from [ 11 C]propionyl chloride prepared from the corresponding Grignard reagent and [ 11 C]carbon dioxide (Figure ) . In the same year, a synthesis of [ 11 C]alfentanil from [ 11 C]iodomethane was reported without mention of the observed specific activity (Figure ) . No PET studies were reported from any of these tracers with only the radiofluorinated analog of fentanyl reporting some results from rodent biodistribution studies.…”

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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Syntheses and Uses of Isotopically Labelled Organic Halides

Zieliński

Kańska

2009

Patai's Chemistry of Functional Groups

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Introduction Syntheses and Uses of Organic Halides Labelled with Fluorine‐18 and Carbon‐11 Syntheses and Uses of Isotopically Labelled Organic Chlorides Syntheses and Applications of Bromine Isotopes Syntheses and Uses of Organic Compounds Labelled with Iodine Isotopes Syntheses of Organic Compounds Labelled with Astatine‐211 Isotope Effect Studies with Organic Halides Acknowledgements

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Studies to label alfentanil with carbon-11

Cited by 3 publications

References 15 publications

PET and SPECT Imaging of the Opioid System: Receptors, Radioligands and Avenues for Drug Discovery and Development

PET and SPECT Imaging of the Opioid System: Receptors, Radioligands and Avenues for Drug Discovery and Development

Positron emission tomography radioligands for the opioid system

Syntheses and Uses of Isotopically Labelled Organic Halides

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