New imide 5-HT1A receptor ligands - modification of terminal fragment geometry

Two sets of new o-methoxyphenylpiperazine (MPP; series a) and 1,2,3,4-tetrahydroisoquinoline (THIQ; series b) derivatives, containing various imide moieties derived from NAN190, were synthesized and evaluated in vitro for their ability to bind to the serotonin 5-HT(1A) and 5-HT(2A) receptors. All ne...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2004-02, Vol.9 (3), p.170-177
Main Authors: Bojarski, Andrzej J, Mokrosz, Maria J, Duszyńska, Beata, Kozioł, Aneta, Bugno, Ryszard
Format: Article
Language:English
Subjects:
4-tetrahydroisoquinoline derivatives
5-HT1A ligands
Animals
arylpiperazine derivatives
Buspirone - analogs & derivatives
Buspirone - chemistry
Geometry
Humans
Ligands
Piperazines - chemical synthesis
Piperazines - chemistry
Piperazines - pharmacology
Serotonin 5-HT1 Receptor Antagonists
Serotonin Antagonists - chemical synthesis
Serotonin Antagonists - chemistry
Serotonin Antagonists - pharmacology
Structure-Activity Relationship
Tetrahydroisoquinolines - chemical synthesis
Tetrahydroisoquinolines - chemistry
Tetrahydroisoquinolines - pharmacology
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Summary:Two sets of new o-methoxyphenylpiperazine (MPP; series a) and 1,2,3,4-tetrahydroisoquinoline (THIQ; series b) derivatives, containing various imide moieties derived from NAN190, were synthesized and evaluated in vitro for their ability to bind to the serotonin 5-HT(1A) and 5-HT(2A) receptors. All new derivatives from series a demonstrated high 5-HT(1A) affinities, whereas THIQ analogues were much less active. With respect to 5-HT(2A) receptors, three MPP derivatives presented moderate activity but the rest of the investigated compounds were practically inactive. The influence of changes in terminus geometry on 5-HT(1A) receptor affinity was analyzed in regard to model compounds NAN190and MM199.
ISSN:1420-3049
1420-3049
DOI:10.3390/90300170