UNIGE document Scientific Article
previous document  unige:73836  next document
add to browser collection
Title

Design of a serotonin 4 receptor radiotracer with decreased lipophilicity for single photon emission computed tomography

Authors
Fresneau, Nathalie
Fossey, Christine
Ballandonne, Céline
Lesnard, Aurélien
show hidden authors show all authors [1 - 11]
Published in European Journal of Medicinal Chemistry. 2015, vol. 94, p. 386-96
Abstract With the aim to develop a suitable radiotracer for the brain imaging of the serotonin 4 receptor subtype (5-HT4R) using single photon emission computed tomography (SPECT), we synthesized and evaluated a library of di- and triazaphenanthridines with lipophilicity values which were in the range expected to favour brain penetration, and which demonstrated specific binding to the target of interest. Adding additional nitrogen atoms to previously described phenanthridine ligands exhibiting a high unspecific binding, we were able to design a radioiodinated compound [(125)I]14. This compound exhibited a binding affinity value of 0.094 nM toward human 5-HT4R and a high selectivity over other serotonin receptor subtypes (5-HTR). In vivo SPECT imaging studies and competition experiments demonstrated that the decreased lipophilicity (in comparison with our previously reported compounds 4 and 5) allowed a more specific labelling of the 5-HT4R brain-containing regions.
Identifiers
PMID: 25778994
Full text
Article (Published version) (1 MB) - document accessible for UNIGE members only Limited access to UNIGE
Structures
Research groups Groupe Giannakopoulos Panteleimon (psychiatrie générale) (201)
Neuroimagerie moléculaire en psychiatrie (983)
Citation
(ISO format)
FRESNEAU, Nathalie et al. Design of a serotonin 4 receptor radiotracer with decreased lipophilicity for single photon emission computed tomography. In: European Journal of Medicinal Chemistry, 2015, vol. 94, p. 386-96. https://archive-ouverte.unige.ch/unige:73836

176 hits

0 download

Update

Deposited on : 2015-07-02

Export document
Format :
Citation style :