Radiosynthesis of [18F]flumazenil for imaging benzodiazepine receptors and its evaluation in human volunteers using simultaneous PET-MRI

Kumar, Pardeep; Nagaraj, Chandana; Joshi, Raman Kumar; Goud, Nerella Sridhar; Kumar, Dilip; Korann, Vittal; Mangalore, Sandhya; Rao, Naren Prahalada

doi:10.1007/s10967-021-07859-w

Cited by 7 publications

(5 citation statements)

References 15 publications

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“…The synthesis of [ 11 C] 28 involves the 11 C-methylation of ethyl 8-fluoro-6-oxo-5,6-dihydro-4 H -benzo[ f ]imidazo[1,5- a ][1,4]diazepine-3-carboxylate (Scheme ). On the other hand, [ 18 F] 28 is synthesized through radiofluorination using boronic ester precursors …”

Section: F- and 11c-labeled Pet Tracers Based On Anestheticsmentioning

confidence: 99%

“…The synthesis of [ 11 C]28 involves the 11 144 On the other hand, [ 18 F]28 is synthesized through radiofluorination using boronic ester precursors. 145 BZDs are commonly used as sedative-hypnotics and anxiolytics. These compounds are characterized by the replacement of the hydrogen on the BZD ring by different groups, resulting in similar basic pharmacological actions of BZD drugs.…”

Section: F-and 11 C-labeled Pet Tracers Based On Anestheticsmentioning

confidence: 99%

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A Molecular Toolbox of Positron Emission Tomography Tracers for General Anesthesia Mechanism Research

Wang

Fan

et al. 2023

J. Med. Chem.

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With appropriate radiotracers, positron emission tomography (PET) allows direct or indirect monitoring of the spatial and temporal distribution of anesthetics, neurotransmitters, and biomarkers, making it an indispensable tool for studying the general anesthesia mechanism. In this Perspective, PET tracers that have been recruited in general anesthesia research are introduced in the following order: 1) 11 C/ 18 F-labeled anesthetics, i.e., PET tracers made from inhaled and intravenous anesthetics; 2) PET tracers targeting anesthesia-related receptors, e.g., neurotransmitters and voltage-gated ion channels; and 3) PET tracers for studying anesthesia-related neurophysiological effects and neurotoxicity. The radiosynthesis, pharmacodynamics, and pharmacokinetics of the above PET tracers are mainly discussed to provide a practical molecular toolbox for radiochemists, anesthesiologists, and those who are interested in general anesthesia.

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Section: F- and 11c-labeled Pet Tracers Based On Anestheticsmentioning

confidence: 99%

Section: F-and 11 C-labeled Pet Tracers Based On Anestheticsmentioning

confidence: 99%

A Molecular Toolbox of Positron Emission Tomography Tracers for General Anesthesia Mechanism Research

Wang

Fan

et al. 2023

J. Med. Chem.

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“…Being a dedicated Neuro Institute, NIMHANS has developed radiotracers such as fluorine-18-[ 18 F] flumazenil for imaging benzodiazepine receptors, [ 18 F]-AVT-011 for assessing p-glycoprotein expression, and also started carbon-11-PBR28 TSPO PET imaging in amyotrophic lateral sclerosis. [ 18 , 19 ]…”

Section: India's Emergence To the Forefront Of The Clinical And Resea...mentioning

confidence: 99%

India's Growing Nuclear Medicine Infrastructure and Emergence of Radiotheranostics in Cancer Care: Associated Challenges and the Opportunities to Collaborate

Singh,

Sahani,

Prasad

et al. 2023

Indian Journal of Nuclear Medicine

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“…The clinically used PET radiotracers like [ 18 F]FDG, 18 F-FLT, 18 F-FES, and 18 F-choline were synthesized using nucleophilic radiofluorination reactions with 18 F-fluoride, from which the synthesis of [ 18 F]FDG was shown in Figure 7B (59). Many automated synthesis modules and methodologies are developed based on nucleophilic radiofluorination (60,61). Recently one study reported first transition metal assisted 18 F-labeling of heteroaromatic phenols through deoxyfluorination process via Ruthenium π-complexes.…”

Section: The Chemistry Of Radiolabeling With Fluorine-18 and Carbon-1...mentioning

confidence: 99%

PET Molecular Imaging in Drug Development: The Imaging and Chemistry Perspective

et al. 2022

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Positron emission tomography with selective radioligands advances the drug discovery and development process by revealing information about target engagement, proof of mechanism, pharmacokinetic and pharmacodynamic profiles. Positron emission tomography (PET) is an essential and highly significant tool to study therapeutic drug development, dose regimen, and the drug plasma concentrations of new drug candidates. Selective radioligands bring up target-specific information in several disease states including cancer, cardiovascular, and neurological conditions by quantifying various rates of biological processes with PET, which are associated with its physiological changes in living subjects, thus it reveals disease progression and also advances the clinical investigation. This study explores the major roles, applications, and advances of PET molecular imaging in drug discovery and development process with a wide range of radiochemistry as well as clinical outcomes of positron-emitting carbon-11 and fluorine-18 radiotracers.

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Radiosynthesis of [18F]flumazenil for imaging benzodiazepine receptors and its evaluation in human volunteers using simultaneous PET-MRI

Cited by 7 publications

References 15 publications

A Molecular Toolbox of Positron Emission Tomography Tracers for General Anesthesia Mechanism Research

A Molecular Toolbox of Positron Emission Tomography Tracers for General Anesthesia Mechanism Research

India's Growing Nuclear Medicine Infrastructure and Emergence of Radiotheranostics in Cancer Care: Associated Challenges and the Opportunities to Collaborate

PET Molecular Imaging in Drug Development: The Imaging and Chemistry Perspective

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