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Chiral aryloxyalkylamines: Selective 5-HT(1B/1D) activation and analgesic activity. 2010
Alessia Carocci, and
Giovanni Lentini, and
Alessia Catalano, and
Maria Maddalena Cavalluzzi, and
Claudio Bruno, and
Marilena Muraglia, and
Nicola Antonio Colabufo, and
Nicoletta Galeotti, and
Filomena Corbo, and
Rosanna Matucci, and
Carla Ghelardini, and
Carlo Franchini
Dipartimento Farmaco-Chimico, Università degli Studi di Bari, Italy. glentini@farmchim.uniba.it <glentini@farmchim.uniba.it>
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 guinea pig assay and showed higher analgesic activity than both sumatriptan and the achiral analogue 20 b in the mouse hot-plate test. Neither ligand displayed any affinity for nicotinic ACh receptors present in mouse brain membranes, thus indicating that their analgesic activity does not arise through interaction with these receptors.
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