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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
* Author to whom correspondence should be addressed.
Received: 14 January 2004 / Accepted: 19 January 2004 / Published: 28 February 2004
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.
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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.
Bojarski AJ, Mokrosz MJ, Duszyńska B, Kozioł A, Bugno R. New Imide 5-HT1A Receptor Ligands – Modification of Terminal Fragment Geometry. Molecules. 2004; 9(3):170-177.
Bojarski, Andrzej J.; Mokrosz, Maria J.; Duszyńska, Beata; Kozioł, Aneta; Bugno, Ryszard. 2004. "New Imide 5-HT1A Receptor Ligands – Modification of Terminal Fragment Geometry." Molecules 9, no. 3: 170-177.