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.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Anxiety / drug therapy
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Depression / drug therapy
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Ligands
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Piperazines / chemistry*
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Piperazines / pharmacology
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Piperazines / therapeutic use
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Quantitative Structure-Activity Relationship
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Receptors, Serotonin / metabolism*
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Receptors, Serotonin, 5-HT1
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Schizophrenia / drug therapy
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Serotonin Antagonists / chemistry*
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Serotonin Antagonists / pharmacology
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Serotonin Antagonists / therapeutic use
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Serotonin Receptor Agonists / chemistry*
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Serotonin Receptor Agonists / pharmacology
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Serotonin Receptor Agonists / therapeutic use
Substances
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Ligands
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Piperazines
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Receptors, Serotonin
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Receptors, Serotonin, 5-HT1
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Serotonin Antagonists
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Serotonin Receptor Agonists