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

Cailly, Thomas; Dumas, Noe; Millet, Philippe; Lemaitre, Stephane; Fabis, Frederic; Charnay, Yves; Rault, Sylvain

doi:10.1016/j.ejmech.2010.07.052

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Title		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
Authors		Cailly, Thomas Dumas, Noe Millet, Philippe Lemaitre, Stephane Fabis, Frederic Charnay, Yves Rault, Sylvain
Published in		European Journal of Medicinal Chemistry. 2010, vol. 45, no. 11, p. 5465-5467
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.
Keywords		Chromatography, High Pressure Liquid — Iodine Radioisotopes/chemistry/diagnostic use — Magnetic Resonance Spectroscopy — Pyrazines/chemical synthesis/diagnostic use — Pyrroles/chemical synthesis/diagnostic use — Thiophenes/chemical synthesis/diagnostic use — *Tomography, Emission-Computed, Single-Photon
Identifiers		DOI: 10.1016/j.ejmech.2010.07.052 PMID: 20817325
Full text		Article - Limited access to UNIGE Other version: http://ac.els-cdn.com/S0223523410005489/1-s2.0-S0223523410005489-main.pdf?_tid=77fedae6e3d9dd6fee42f572b2ea4fcd&acdna...
Structures		Faculté de médecine / Section de médecine clinique / Département de psychiatrie
Research group		Neuroimagerie moléculaire en psychiatrie (983)
Citation (ISO format)		CAILLY, Thomas et al. 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. In: European Journal of Medicinal Chemistry, 2010, vol. 45, n° 11, p. 5465-5467. doi: 10.1016/j.ejmech.2010.07.052 https://archive-ouverte.unige.ch/unige:20817

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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