Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5991
Title: Bivalent Ligands for the Serotonin 5-HT3 Receptor
Authors: Cappelli, Andrea 
Manini, Monica
Paolino, Marco 
A., Gallelli
Anzini, Maurizio 
L., Mennuni
M., DEL CADIA
F., DE RIENZO
M. C., Menziani
Vomero, Salvatore
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.
Description: 
36919
URI: http://hdl.handle.net/20.500.12779/5991
ISSN: 1948-5875
DOI: 10.1021/ml2000388
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