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

Scientific article

English

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

ContributorsCailly, Thomas; Dumas, Noe; Millet, Philippe

; Lemaitre, Stephane; Fabis, Frederic; Charnay, Yves; Rault, Sylvain

Published inEuropean journal of medicinal chemistry, vol. 45, no. 11, p. 5465-5467

Publication date2010

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

Affiliation

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

Article

Identifiers

PID : unige:20817
DOI : 10.1016/j.ejmech.2010.07.052
PMID : 20817325

Commercial URLhttp://ac.els-cdn.com/S0223523410005489/1-s2.0-S0223523410005489-main.pdf?_tid=77fedae6e3d9dd6fee42f572b2ea4fcd&acdnat=1335965972_06d154be90645b35f59cb0af9d6b4308

ISSN of the journal0223-5234

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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

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