Chemistry of β +-Emitting Compounds Based on Fluorine-18
The aim of this review is to emphasise the scopes and limitations of the chemistry with fluorine-18 and the potential applications of the new 18F-radiopharmaceuticals are reviewed.
PET and SPECT imaging of the NMDA receptor system: an overview of radiotracer development.
- F. Sobrio, G. Gilbert, C. Perrio, L. Barré, D. Debruyne
- Medicine, BiologyMini reviews in medicinal chemistry
- 31 July 2010
To assess NMDAR radiotracer development and to propose perspectives, the PET and SPECT candidate radioligands developed until now were overviewed and labelled molecules of interest were classified according to their binding site.
Microspheres based on inulin for the controlled release of serine protease inhibitors: preparation, characterization and in vitro release.
[11C]-MeJDTic: a novel radioligand for kappa-opioid receptor positron emission tomography imaging.
Chemical delivery system of metaiodobenzylguanidine (MIBG) to the central nervous system.
- F. Gourand, Guillaume Mercey, L. Barré
- Biology, ChemistryJournal of medicinal chemistry
- 19 January 2010
The synthesis to link 4 to the chemical delivery system and the radiosynthesis with carbon-11 of the "CDS-4 entity" is reported, and the release of 4 into the CNS is confirmed.
Functionalization through lithiation of (S)-N-(1-phenylpropyl)-2-phenylquinoline-4-carboxamide. Application to the labeling with carbon-11 of NK-3 receptor antagonist SB 222200.
The 3-trimethylstannyl derivative was subjected to a Stille reaction using methyl, phenyl, or thienyliodide to afford the alkyl or aryl quinolines in moderate to good yields.
Synthesis and in Vitro Characterisation of Ifenprodil‐Based Fluorescein Conjugates as GluN1/GluN2B N‐Methyl‐D‐aspartate Receptor Antagonists
- M. Dhilly, Javier Becerril-Ortega, C. Perrio
- Biology, ChemistryChembiochem : a European journal of chemical…
- 15 April 2013
Fluorescent probes to target the GluN2B subunit selectively in order to allow better understanding of the relationships between receptor localisation and physiological importance had a neuroprotective effect equivalent to that of ifenprodil in a standard test for neurotoxicity, and it was demonstrated that they displaced [3H]ifenproDil in mouse brain slices in a similar manner.
Multimodal evaluation of hypoxia in brain metastases of lung cancer and interest of hypoxia image-guided radiotherapy
Hypoxia is a major yet heterogeneous feature of BM from lung cancer both preclinically and clinically and HIGRT, based on hypoxia heterogeneity observed between cortical and striatal metastases in the intracerebrally induced models, showed significant potential for tumor control and animal survival.
Lithiation of Functionalized Fluoroquinolines: Synthesis of Dihalo‐2‐phenylquinoline‐4‐carboxamides and in vitro Evaluation as NK‐3 Receptor Ligands for Medical Imaging Studies.
Copper-catalyzed amination of (bromophenyl)ethanolamine for a concise synthesis of aniline-containing analogues of NMDA NR2B antagonist ifenprodil.
- Cédric Bouteiller, Javier Becerril-Ortega, C. Perrio
- Chemistry, BiologyOrganic & biomolecular chemistry
- 18 February 2010
An operationally simple and concise synthesis of anilinoethanolamines, as NMDA NR2B receptor antagonist ifenprodil analogues, was developed via a copper-catalyzed amination of the corresponding bromoarene using CuI and N,N-diethylsalicylamide, 2,4-pentadione or 2-acetylcyclohexanone as catalytic systems.