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Open AccessArticle

New Imide 5-HT1A Receptor Ligands – Modification of Terminal Fragment Geometry

Department of Medicinal Chemistry, Institute of Pharmacology of the Polish Academy of Sciences, 12 Smętna Street, 31-343 Kraków, Poland
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Molecules 2004, 9(3), 170-177; https://doi.org/10.3390/90300170
Received: 14 January 2004 / Accepted: 19 January 2004 / Published: 28 February 2004
(This article belongs to the Special Issue Biologically Relevant Heterocyclic Compounds)
Two sets of new o-methoxyphenylpiperazine (MPP; series a) and 1,2,3,4-tetrahydroisoquinoline (THIQ; series b) derivatives, containing various imide moietiesderived from NAN190, were synthesized and evaluated in vitro for their ability to bind tothe serotonin 5-HT1A and 5-HT2A receptors. All new derivatives from series a demonstratedhigh 5-HT1A affinities, whereas THIQ analogues were much less active. With respect to5-HT2A receptors, three MPP derivatives presented moderate activity but the rest of theinvestigated compounds were practically inactive. The influence of changes in terminusgeometry on 5-HT1A receptor affinity was analyzed in regard to model compounds NAN190and MM199. View Full-Text
Keywords: 5-HT1A ligands; arylpiperazine derivatives; 1; 2; 3; 4-tetrahydroisoquinoline derivatives. 5-HT1A ligands; arylpiperazine derivatives; 1; 2; 3; 4-tetrahydroisoquinoline derivatives.
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Bojarski, A.J.; Mokrosz, M.J.; Duszyńska, B.; Kozioł, A.; Bugno, R. New Imide 5-HT1A Receptor Ligands – Modification of Terminal Fragment Geometry. Molecules 2004, 9, 170-177.

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