5-HT1A AND 5-HT2A RECEPTOR AFFINITY AND FUNCTIONAL PROFILE OF SOME N-[3-(4-ARYL-1-PIPERAZINYL)PROPYL] DERIVATIVES OF INDOLIN-2(1H)-ONE, QUINOLIN-2(1H)ONE AND ISOQUINOLIN-1(2H)-ONE .30. STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF CNS AGENTS

Authors
MOKROSZ MJ MOKROSZ JL DUSZYNSKA B DERENWESOLEK A KLODZINSKA A KOWALSKI P CHARAKCHIEVAMINOL S TATARCZYNSKA E KOWALSKA T MAJKA Z CHOJNACKAWOJCIK E MISZTAL S
Citation
Mj. Mokrosz et al., 5-HT1A AND 5-HT2A RECEPTOR AFFINITY AND FUNCTIONAL PROFILE OF SOME N-[3-(4-ARYL-1-PIPERAZINYL)PROPYL] DERIVATIVES OF INDOLIN-2(1H)-ONE, QUINOLIN-2(1H)ONE AND ISOQUINOLIN-1(2H)-ONE .30. STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF CNS AGENTS, Die Pharmazie, 52(6), 1997, pp. 423-428
Citations number
18
Categorie Soggetti
Pharmacology & Pharmacy",Chemistry
Journal title
Die Pharmazie → ACNP
ISSN journal
00317144
Volume
52
Issue
6
Year of publication
1997
Pages
423 - 428
Database
ISI
SICI code
0031-7144(1997)52:6<423:5A5RAA>2.0.ZU;2-P
Abstract
A series of new 1-aryl-4-propylpiperazines containing the modified ter minal amide fragment 9, 15-19, 21, 23 and 25 were synthesized and thei r 5-HT1A and 5-HT2A receptor affinities were determined. All the compo und were highly potent 5-HT1A receptor ligands with a diverse 5-HT2A r eceptor affinity. It was found that the 5-HT2A receptor affinity depen ds on the dipole moment and lipophilicity of amide moiety. Compound 9b was found to be a 5-HT2A receptor antagonist and a weak 5-HT1A recept or agonist.