2. Academic Validation
  3. New imide 5-HT1A receptor ligands - modification of terminal fragment geometry

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

  • Molecules. 2004 Feb 28;9(3):170-7. doi: 10.3390/90300170.
Andrzej J Bojarski 1,  Maria J Mokrosz,  Beata Duszyńska,  Aneta Kozioł,  Ryszard Bugno
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Institute of Pharmacology of the Polish Academy of Sciences, 12 Smetna Street, 31-343 Kraków, Poland. bojarski@if-pan.krakow.pl
PMID: 18007421 DOI: 10.3390/90300170
Abstract

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.

Figures
Products