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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
- Source :
- European Journal of Medicinal Chemistry, European Journal of Medicinal Chemistry, Elsevier, 2010, 45 (11), pp.5465-5467, European Journal of Medicinal Chemistry, Vol. 45, No 11 (2010) pp. 5465-5467, European journal of medicinal chemistry
- Publication Year :
- 2010
- Publisher :
- HAL CCSD, 2010.
-
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.
- 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
Subjects
Details
- Language :
- English
- ISSN :
- 02235234 and 17683254
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry, European Journal of Medicinal Chemistry, Elsevier, 2010, 45 (11), pp.5465-5467, European Journal of Medicinal Chemistry, Vol. 45, No 11 (2010) pp. 5465-5467, European journal of medicinal chemistry
- Accession number :
- edsair.doi.dedup.....702e1422b6da03e01fee14ff0305be7f