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

Andrzej Bojarski, Maria Mokrosz, Beata Duszyńska, Aneta Kozioł, Ryszard Bugno
2004 Molecules  
Two sets of new o-methoxyphenylpiperazine (MPP; series a) and 1,2,3,4tetrahydroisoquinoline (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
more » ... e 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 NAN190 and MM199.
doi:10.3390/90300170 pmid:18007421 fatcat:bjhoaexluzhgtjhg5iwjpd6p5e