1. Synthesis and characterization of a iodine-125-labeled pyrrolo[1,2-a]thieno[3,2-e]pyrazine and evaluation as a potential 5-HT4R SPECT tracer
- Author
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Philippe Millet, Thomas Cailly, Yves Charnay, Stephane Lemaitre, Frédéric Fabis, Sylvain Rault, Noé Dumas, Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Normandie Université (NU), Hôpitaux Universitaires de Genève (HUG), Embedded System Lab (ESL), Thales Research and Technology, and Cailly, Thomas
- Subjects
Tomography, Emission-Computed, Single-Photon ,Magnetic Resonance Spectroscopy ,Pyrazine ,Stereochemistry ,[CHIM.THER] Chemical Sciences/Medicinal Chemistry ,chemistry.chemical_element ,Thiophenes ,[CHIM.THER]Chemical Sciences/Medicinal Chemistry ,Iodine ,Chemical synthesis ,Iodine Radioisotopes/*chemistry/*diagnostic use ,Iodine Radioisotopes ,03 medical and health sciences ,chemistry.chemical_compound ,ddc:616.89 ,0302 clinical medicine ,Drug Discovery ,Pyrroles ,Receptor ,Pyrazines/*chemical synthesis/*diagnostic use ,5-HT receptor ,Chromatography, High Pressure Liquid ,ComputingMilieux_MISCELLANEOUS ,030304 developmental biology ,Pharmacology ,0303 health sciences ,Organic Chemistry ,Radiochemistry ,General Medicine ,Pyrroles/*chemical synthesis/*diagnostic use ,Ligand (biochemistry) ,Thiophenes/*chemical synthesis/*diagnostic use ,3. Good health ,chemistry ,Pyrazines ,030217 neurology & neurosurgery ,Preclinical imaging ,Ex vivo - Abstract
In the aim to find new radiotracers for the in vivo imaging of 5-HT(4) receptors by ultra-high resolution quantitative SPECT, we have developed the synthesis of a radioiodinated 5-HT(4) ligand using an iododestannylation procedure. The [(125)I]-ligand was obtained in a high radiochemical yield. Preliminary autoradiographic and ex vivo studies failed to show a specific labeling of 5-HT(4) receptors.
- Published
- 2010