Novel potent 5-HT(3) receptor ligands based on the pyrrolidone structure. Effects of the quaternization of the basic nitrogen on the interaction with 5-HT(3) receptor

The results of a comprehensive structure-affinity relationship study on the effect of the quaternization (i.e., N-methylation) of structurally different ligands in the classes of tropane and quinuclidine derivatives are described. This study shows that the effects of the quaternization of the basic...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2002-08, Vol.10 (8), p.2681-2691
Hauptverfasser:	Cappelli, Andrea, Gallelli, Andrea, Braile, Carlo, Anzini, Maurizio, Vomero, Salvatore, Mennuni, Laura, Makovec, Francesco, Menziani, M Cristina, De Benedetti, Pier G, Donati, Alessandro, Giorgi, Gianluca
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Brain - cytology Brain - metabolism Crystallography, X-Ray Ligands Magnetic Resonance Spectroscopy Male Molecular Structure Protein Binding Pyrrolidinones - chemical synthesis Pyrrolidinones - pharmacology Quaternary Ammonium Compounds Quinuclidines - chemical synthesis Quinuclidines - pharmacology Rats Rats, Wistar Receptors, Serotonin - chemistry Receptors, Serotonin, 5-HT3 Serotonin Antagonists - chemical synthesis Structure-Activity Relationship Tropanes - chemical synthesis Tropanes - pharmacology
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