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|Title:||Bivalent Ligands for the Serotonin 5-HT3 Receptor||Authors:||Cappelli, Andrea
M., DEL CADIA
F., DE RIENZO
M. C., Menziani
|Issue Date:||2011||Project:||None||Journal:||ACS MEDICINAL CHEMISTRY LETTERS||Abstract:||
The serotonin 5-HT3 receptor is a ligand-gatedion channel, which by virtue of its pentameric architecture, canbe considered to be an intriguing example of intrinsicallymultivalent biological receptors. This paper describes a generaldesign approach to the study of multivalency in this multimericion channel. Bivalent ligands for 5-HT3 receptor have beendesigned by linking an arylpiperazine moiety to probes showingdifferent functional features. Both homobivalent and heterobivalentligands have shown 5-HT3 receptor affinity in thenanomolar range, providing evidence for the viability of ourdesign approach. Moreover, the high affinity shown by homobivalentligands suggests that bivalency is a promising approachin 5-HT3 receptor modulation and provides the rational basis for applying the concepts of multivalency to the study of 5-HT3receptor function.
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