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ID: ALA1136702
Journal: Bioorg Med Chem Lett
Title: 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-HT1A receptor agonist.
Authors: López-Rodríguez ML, Morcillo MJ, Fernández E, Benhamú B, Tejada I, Ayala D, Viso A, Olivella M, Pardo L, Delgado M, Manzanares J, Fuentes JA.
Abstract: Based on a computational model for 5-HT(1A)R-ligand interaction and QSAR studies, we have designed and synthesized a new series of arylpiperazines 2-8 which exhibit high 5-HT(1A)R affinity and selectivity over alpha(1)-adrenergic receptors. Among them, compound CSP-2503 (4) has been pharmacologically characterized as a 5-HT(1A)R agonist at somatodendritic and postsynaptic sites, endowed with anxiolytic properties.
CiteXplore: 12668005