Abstract
The selectivity for 5-HT(1A) versus D(4) receptors is significantly increased when the basic side chain of WAY-100635 is replaced by a 4-phenylpiperazine (3e) or a 4-phenyl-1,2,3,6-tetrahydropyridine moiety (3i). The 4-phenyl-1,2,3,6-tetrahydropyridine compounds (3i-l) have a higher affinity for 5-HT(1A) receptors than do the corresponding unsubstituted phenylpiperazine analogues (3e-h). Compounds 3e and 3i appear to be selective for 5-HT(1A) receptors over other relevant receptors and still behave as neutral antagonists.
Copyright © 2012 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Molecular Structure
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Piperazines / chemistry*
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Piperazines / pharmacology
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Pyridines / chemistry*
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Pyridines / pharmacology
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Receptor, Serotonin, 5-HT1A / metabolism
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Receptors, Dopamine D4 / antagonists & inhibitors*
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Receptors, Dopamine D4 / metabolism
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Serotonin 5-HT1 Receptor Antagonists / chemistry*
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Serotonin 5-HT1 Receptor Antagonists / pharmacology
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Structure-Activity Relationship
Substances
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Piperazines
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Pyridines
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Serotonin 5-HT1 Receptor Antagonists
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Receptor, Serotonin, 5-HT1A
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Receptors, Dopamine D4
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N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide