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Molecules 2004, 9(3), 170-177; doi:10.3390/90300170
Article

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

* , , ,  and
Department of Medicinal Chemistry, Institute of Pharmacology of the Polish Academy of Sciences, 12 Smętna Street, 31-343 Kraków, Poland
* Author to whom correspondence should be addressed.
Received: 14 January 2004 / Accepted: 19 January 2004 / Published: 28 February 2004
(This article belongs to the Special Issue Biologically Relevant Heterocyclic Compounds)
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Abstract

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.
Keywords: 5-HT1A ligands; arylpiperazine derivatives; 1; 2; 3; 4-tetrahydroisoquinoline derivatives. 5-HT1A ligands; arylpiperazine derivatives; 1; 2; 3; 4-tetrahydroisoquinoline derivatives.
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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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