Abstract
A series of new arylpiperazine derivatives 2, which are devoid of the terminal amide fragment present in related 5-HT1A ligands, was prepared and evaluated for affinity at 5-HT1A and alpha 1 receptors. All the compounds 2 demonstrated high affinity for the 5-HT1A receptor and moderate affinity for alpha 1 receptor binding sites. Structure-activity relationship (SAR) studies suggest that there is influence of electronic factors on the no-pharmacophoric part of the alpha 1 receptor site. However there is no influence of electronic interactions on the stabilization of the 5-HT1A receptor-ligand complex.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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8-Hydroxy-2-(di-n-propylamino)tetralin / metabolism
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Animals
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Antihypertensive Agents / metabolism
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Cerebral Cortex / metabolism
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In Vitro Techniques
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Models, Chemical
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Piperazines / chemistry*
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Piperazines / pharmacology
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Prazosin / metabolism
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Rats
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Receptors, Serotonin / metabolism*
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Receptors, Serotonin, 5-HT1
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Serotonin Receptor Agonists / metabolism
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Structure-Activity Relationship
Substances
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Antihypertensive Agents
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Piperazines
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Receptors, Serotonin
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Receptors, Serotonin, 5-HT1
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Serotonin Receptor Agonists
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8-Hydroxy-2-(di-n-propylamino)tetralin
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Prazosin