Abstract
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
Current Medicinal Chemistry
Title: Arylpiperazine Derivatives Acting at 5-HT1A Receptors
Volume: 9 Issue: 4
Author(s): M. L. Lopez-Rodriguez, D. Ayala, B. Benhamu, M. J. Morcillo and A. Viso
Affiliation:
Keywords: Arylpiperazine Derivatives, 5-hydroxytryptamine, aryloxyalkylamines and arylpiperazines, Antagonist Pharmacophore, postsynaptic receptor sites, alpha-carbon coordinate
Abstract: 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.
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Cite this article as:
Lopez-Rodriguez L. M., Ayala D., Benhamu B., Morcillo J. M. and Viso A., Arylpiperazine Derivatives Acting at 5-HT1A Receptors, Current Medicinal Chemistry 2002; 9 (4) . https://dx.doi.org/10.2174/0929867023371030
DOI https://dx.doi.org/10.2174/0929867023371030 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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