Design and synthesis of S-(-)-2-[[4-(napht-1-yl)piperazin-1-yl]methyl]-1,4-dioxoperhydropyrrolo[1,2- a]pyrazine (CSP-2503) using computational simulation. A 5-HT<inf>1A</inf> receptor agonist

María L. López-Rodríguez, Ma José Morcillo, Esther Fernández, Bellinda Benhamú, Ignacio Tejada, David Ayala, Alma Viso, Mireia Olivella, Leonardo Pardo, Mercedes Delgado, Jorge Manzanares, José A. Fuentes

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20 Citations (Scopus)

Abstract

Based on a computational model for 5-HT1AR-ligand interaction and QSAR studies, we have designed and synthesized a new series of arylpiperazines 2-8 which exhibit high 5-HT1AR affinity and selectivity over α1-adrenergic receptors. Among them, compound CSP-2503 (4) has been pharmacologically characterized as a 5-HT1AR agonist at somatodendritic and postsynaptic sites, endowed with anxiolytic properties. © 2003 Elsevier Science Ltd. All rights reserved.
Original languageEnglish
Pages (from-to)1429-1432
JournalBioorganic and Medicinal Chemistry Letters
Volume13
Issue number8
DOIs
Publication statusPublished - 17 Apr 2003

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