Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine …

…, F Makovec, E Doucet, M Hamon, G Bruni…

Index: Cappelli, Andrea; Anzini, Maurizio; Vomero, Salvatore; Mennuni, Laura; Makovec, Francesco; Doucet, Edith; Hamon, Michel; Bruni, Giancarlo; Romeo, Maria R.; Menziani, M. Cristina; De Benedetti, Pier G.; Langer, Thierry Journal of Medicinal Chemistry, 1998 , vol. 41, # 5 p. 728 - 741

Full Text: HTML

Citation Number: 71

Abstract

Synthesis and pharmacological evaluation of a series of condensed quinoline and pyridine derivatives bearing a N-methylpiperazine moiety attached to the 2-position of the quinoline or pyridine nucleus are described. 5-HT receptor binding studies revealed subnanomolar affinity for the 5-HT3 receptor subtype in some of the compounds under study. The most active compound (5b) displayed a K i value about 1 order of magnitude higher than that of ...