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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Arylpiperazine Derivatives Acting at 5-HT1A Receptors

Author(s): M. L. Lopez-Rodriguez, D. Ayala, B. Benhamu, M. J. Morcillo and A. Viso

Volume 9 , Issue 4 , 2002

Page: [443 - 469] Pages: 27

DOI: 10.2174/0929867023371030

Price: $65


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.

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

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