Abstract
The synthesis of three 1-[4-(4-aryl-1-piperazinyl)butyl]-3,4-dihydro-2(1H)-quinolinones (5-7) was described and the receptor binding profile (5-HT1A, 5-HT2, alpha 1, D1, D2) was determined. It was found that m-chloro (5) and o-methoxy (6) derivatives are potent antagonists of the 5-HT1A, 5-HT2 and D2 receptors. It was shown that compound 6 resembles very well some atypical antipsychotics and may be considered as a novel agent of this class of drugs.
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 / pharmacology
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Animals
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Antipsychotic Agents / chemical synthesis*
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Antipsychotic Agents / pharmacology
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Behavior, Animal / drug effects
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Central Nervous System Stimulants / pharmacology
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Dextroamphetamine / pharmacology
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Dopamine D2 Receptor Antagonists*
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In Vitro Techniques
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Male
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Motor Activity / drug effects
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Quinolones / chemical synthesis*
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Quinolones / pharmacology
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Rats
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Rats, Wistar
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Receptors, Adrenergic, alpha-1 / drug effects
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Receptors, Dopamine D1 / drug effects
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Reserpine / pharmacology
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Serotonin Antagonists / pharmacology*
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Tryptamines / pharmacology
Substances
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Antipsychotic Agents
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Central Nervous System Stimulants
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Dopamine D2 Receptor Antagonists
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Quinolones
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Receptors, Adrenergic, alpha-1
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Receptors, Dopamine D1
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Serotonin Antagonists
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Tryptamines
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8-Hydroxy-2-(di-n-propylamino)tetralin
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Reserpine
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Dextroamphetamine