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.
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.
Mokrosz
J L
JL
Department of Medicinal Chemistry, Polish Academy of Sciences, Kraków.
Chojnacka-Wójcik
E
E
Dereń-Wesołek
A
A
Kłodzińska
A
A
Maćkowiak
M
M
Bielecka
Z
Z
Paluchowska
M H
MH
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin / Q000494:pharmacology; D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects; D000697:Central Nervous System Stimulants / Q000494:pharmacology; D003913:Dextroamphetamine / Q000494:pharmacology; D065127:Dopamine D2 Receptor Antagonists; D066298:In Vitro Techniques; D008297:Male; D009043:Motor Activity / Q000187:drug effects; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D018340:Receptors, Adrenergic, alpha-1 / Q000187:drug effects; D017447:Receptors, Dopamine D1 / Q000187:drug effects; D012110:Reserpine / Q000494:pharmacology; D012702:Serotonin Antagonists / Q000494:pharmacology*; D014363:Tryptamines / Q000494:pharmacology
D014150:Antipsychotic Agents; D000697:Central Nervous System Stimulants; D065127:Dopamine D2 Receptor Antagonists; D015363:Quinolones; D018340:Receptors, Adrenergic, alpha-1; D017447:Receptors, Dopamine D1; D012702:Serotonin Antagonists; D014363:Tryptamines; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D012110:Reserpine; D003913:Dextroamphetamine