New imide 5-HT1A receptor ligands -: Modification of terminal fragment geometry

被引：16

作者：

Bojarski, AJ ^{[1
]}

Mokrosz, MJ ^{[1
]}

Duszynska, B ^{[1
]}

Koziol, A ^{[1
]}

Bugno, R ^{[1
]}

机构：

[1] Polish Acad Sci, Inst Pharmacol, Dept Med Chem, PL-31343 Krakow, Poland

来源：

MOLECULES | 2004年 / 9卷 / 03期

关键词：

5-HT1A ligands; arylpiperazine derivatives; 1,2,3,4-tetrahydroisoquinoline derivatives;

D O I：

10.3390/90300170

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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-HT1A and 5-HT2A receptors. All new derivatives from series a demonstrated high 5-HT1A affinities, whereas THIQ analogues were much less active. With respect to 5-HT2A 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-HT1A receptor affinity was analyzed in regard to model compounds NAN 190 and MM199.

引用

页码：170 / 177

页数：8

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