Abstract
A new set of 4-alkyl-1-(o-methoxyphenyl)piperazines containing a terminal benzotriazole fragment were synthesized, and their 5-HT1A and 5-HT2 affinity was determined. It was shown that the benzotriazole moiety contributes to both the 5-HT1A and 5-HT2 receptor affinity. It was demonstrated in several behavioral models that 4-[3-(benzotriazol-1- yl)propyl]-1-(2-methoxyphenyl)piperazine (11) is a new, potent presynaptic and postsynaptic 5-HT1A receptor antagonist. However, it is not selective for 5-HT1A versus alpha 1 receptors.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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8-Hydroxy-2-(di-n-propylamino)tetralin / pharmacology
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Animals
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Body Temperature Regulation / drug effects
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Brain / metabolism*
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Indicators and Reagents
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Mice
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Molecular Structure
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Motor Activity / drug effects*
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Piperazines / chemical synthesis*
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Piperazines / chemistry
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Piperazines / pharmacology*
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Posture*
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Radioligand Assay
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Rats
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Receptors, Serotonin, 5-HT1
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Reserpine / pharmacology
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Serotonin Antagonists*
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Stereotyped Behavior / drug effects
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Structure-Activity Relationship
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Triazoles / chemical synthesis*
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Triazoles / chemistry
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Triazoles / pharmacology*
Substances
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Indicators and Reagents
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Piperazines
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Receptors, Serotonin, 5-HT1
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Serotonin Antagonists
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Triazoles
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4-(3-(benzotriazol-1-yl)propyl)-1-(2-methoxyphenyl)piperazine
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8-Hydroxy-2-(di-n-propylamino)tetralin
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Reserpine