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

Molecules

关键词: 5-HT1A ligands;    arylpiperazine derivatives;    1;    2;    3;    4-tetrahydroisoquinoline derivatives.;   

DOI  :  10.3390/90300170

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown