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1. Structure-activity relationship studies of CNS agents. XII. 1-[4-(4-aryl-1-piperazinyl)butyl]-3,4-dihydro-2(1H)-quinolinones: new 5-HT1A, 5-HT2 and D2 ligands with a potential antipsychotic activity.

Author

Mokrosz JL, Chojnacka-Wójcik E, Dereń-Wesołek A, Kłodzińska A, Maćkowiak M, Bielecka Z, and Paluchowska MH

Subjects
8-Hydroxy-2-(di-n-propylamino)tetralin pharmacology, Animals, Antipsychotic Agents pharmacology, Behavior, Animal drug effects, Central Nervous System Stimulants pharmacology, Dextroamphetamine pharmacology, In Vitro Techniques, Male, Motor Activity drug effects, Quinolones pharmacology, Rats, Rats, Wistar, Receptors, Adrenergic, alpha-1 drug effects, Receptors, Dopamine D1 drug effects, Reserpine pharmacology, Tryptamines pharmacology, Antipsychotic Agents chemical synthesis, Dopamine D2 Receptor Antagonists, Quinolones chemical synthesis, Serotonin Antagonists pharmacology
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.

Published
1994

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