Chiral Aryloxyalkylamines: Selective 5??HT1B/1D Activation and Analgesic Activity

…, F Corbo, R Matucci, C Ghelardini, C Franchini

Index: Carocci, Alessia; Lentini, Giovanni; Catalano, Alessia; Cavalluzzi, Maria Maddalena; Bruno, Claudio; Muraglia, Marilena; Colabufo, Nicola Antonio; Galeotti, Nicoletta; Corbo, Filomena; Matucci, Rosanna; Ghelardini, Carla; Franchini, Carlo ChemMedChem, 2010 , vol. 5, # 5 p. 696 - 704

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Citation Number: 9

Abstract

Abstract A series of chiral 2, 3-dichlorophenoxy and 1-naphthyloxy alkylamines were synthesized, and their binding affinities towards 5-HT 1D and h5-HT 1B receptors were evaluated. In the naphthyloxy series, the (R)-prolinol derivative was the most selective 5-HT 1D ligand, while (S)-N-methyl-2-(1-naphthyloxy) propan-1-amine showed the highest selectivity for h5-HT 1B. Both compounds performed as 5-HT 1D agonists in the isolated ...