Purpose: [(18)F]ML-10 is the most advanced radiopharmaceutical for the clinical imaging of the apoptosis phenomenon by PET. The preparation of this radiopharmaceutical on a commercial radiosynthesis module and the requested quality controls for its release are presented herein.
Procedures: ML-10 as reference and its mesyloxy derivative as precursor for labelling with fluorine-18 were prepared. [(18)F]ML-10 was synthesized via a [(18)F]fluorine-de-mesyloxy aliphatic nucleophilic substitution via a GE TRACERLab® FX-FN module. Quality controls were performed.
Results: The labelling precursor was obtained in a four step synthesis in 28 % overall yield affording ML-10 in two steps (88 % yield). Pure [(18)F]ML-10 was obtained with a decay corrected yield of 39.8 % ± 8.4 % (n = 7) in 70 min and a specific activity of 235 ± 85 GBq/μmol at the end of synthesis.
Conclusions: [(18)F]ML-10 was prepared on a widely available automated module and passed the quality control. A LC/MS method was developed to measure specific radioactivity.
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http://dx.doi.org/10.1007/s11307-012-0574-y | DOI Listing |
Pharmaceuticals (Basel)
January 2024
Institut für Pharmazeutische und Medizinische Chemie, Universität Münster, Corrensstraße 48, D-48149 Münster, Germany.
σ receptors play a crucial role in various neurological and neurodegenerative diseases including pain, psychosis, Alzheimer's disease, and depression. Spirocyclic piperidines represent a promising class of potent σ receptor ligands. The relationship between structural modifications and σ receptor affinity and selectivity over σ receptors led to the 2-fluoroethyl derivative fluspidine (, = 0.
View Article and Find Full Text PDFMol Imaging Biol
October 2022
AbbVie Inc., 1 North Waukegan Rd., North Chicago, IL, 60064, USA.
Purpose: Bruton's tyrosine kinase (BTK) is a key component of B cell receptor (BCR) signaling, and as such a critical regulator of cell proliferation and survival. Aberrant BCR signaling is important in the pathogenesis of various B cell malignancies and autoimmune disorders. Here, we describe the development of a novel positron emission tomography (PET) tracer for imaging BTK expression and/or occupancy by small molecule therapeutics.
View Article and Find Full Text PDFJ Am Chem Soc
May 2021
Department of Radiology, University of Michigan, Ann Arbor, Michigan 48109, United States.
This article describes a sequential Ir/Cu-mediated process for the selective C-H radiofluorination of (hetero)arene substrates. In the first step, Ir-catalyzed C(sp)-H borylation affords (hetero)aryl pinacolboronate (BPin) esters. The intermediate organoboronates are then directly subjected to copper-mediated radiofluorination with [F]tetrabutylammonium fluoride to afford fluorine-18 labeled (hetero)arenes in high radiochemical yield and radiochemical purity.
View Article and Find Full Text PDFEJNMMI Radiopharm Chem
November 2020
CERRP, 37100, Tours, France.
Background: Fluorine labelled 8-((E)-4-fluoro-but-2-enyl)-3β-p-tolyl-8-aza-bicyclo[3.2.1]octane-2β-carboxylic acid methyl ester ([F]LBT999) is a selective radioligand for the in vivo neuroimaging and quantification of the dopamine transporter by Positron Emission Tomography (PET).
View Article and Find Full Text PDFJ Labelled Comp Radiopharm
March 2019
Departamento de Radiología y Medicina Física. Centro de Investigaciones Médico-Sanitarias, Universidad de Málaga, Málaga, Spain.
The interest in gallium-68 labelled positron-emission tomography probes continues to increase around the world. However, one of the barriers for routine clinical use is the cost of the automated synthesis units for relatively simple labelling procedures. Herein, we describe the adaptation of a TRACERlab FX synthesis module for the automated production of gallium-68 radiopharmaceuticals using a cation-exchange cartridge for postprocessing of the Ge/ Ga generator eluate.
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