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

Thomas Cailly; Noé Dumas; Philippe Millet; Stéphane Lemaître; Frédéric Fabis; Yves Charnay; Sylvain Rault

doi:10.1016/j.ejmech.2010.07.052

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

Eur J Med Chem. 2010 Nov;45(11):5465-7. doi: 10.1016/j.ejmech.2010.07.052. Epub 2010 Aug 14.

Authors

Thomas Cailly¹, Noé Dumas, Philippe Millet, Stéphane Lemaître, Frédéric Fabis, Yves Charnay, Sylvain Rault

Affiliation

¹ Centre d'Etudes et de Recherche sur le Médicament de Normandie, UPRES EA 4258, INC3M FR-CNRS 3038, UFR des Sciences Pharmaceutiques, Université de Caen Basse-Normandie, boulevard Becquerel 14032 Caen cedex, France.

PMID: 20817325
DOI: 10.1016/j.ejmech.2010.07.052

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.

MeSH terms

Chromatography, High Pressure Liquid
Iodine Radioisotopes / chemistry*
Magnetic Resonance Spectroscopy
Pyrazines / chemical synthesis*
Pyrroles / chemical synthesis*
Thiophenes / chemical synthesis*
Tomography, Emission-Computed, Single-Photon*

Substances

Iodine Radioisotopes
Pyrazines
Pyrroles
Thiophenes