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Arylpiperazine Derivatives Acting at 5-HT1A Receptors

[ Vol. 9 , Issue. 4 ]


M. L. Lopez-Rodriguez, D. Ayala, B. Benhamu, M. J. Morcillo and A. Viso   Pages 443 - 469 ( 27 )


Serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists. Among 5-HTRs, the 5-HT 1A subtype is the best studied and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind 5-HT 1A R sites. Among these, arylpiperazine derivatives represent one of the most important classes of 5-HT 1A R ligands. This article will review the development of arylpiperazine derivatives acting at 5-HT 1A Rs with an emphasis on structure-affinity relationships of agonists and antagonists, ligand-receptor interactions and pharmacological applications.


Arylpiperazine Derivatives,5-hydroxytryptamine,aryloxyalkylamines and arylpiperazines,Antagonist Pharmacophore,postsynaptic receptor sites,alpha-carbon coordinate


, , , , Departamento de QuimicaOrganica I, Facultad de Ciencias Quimicas, Universidad Complutense, E-28040 Madrid, Spain

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