Arylpiperazine derivatives of 3-propyl-β-tetralonohydantoin as new 5-HT1A and 5-HT2A receptor ligands

被引：0
|
作者：
Byrtus, H
Pawlowski, M
Duszynska, B
Wesolowska, A
Chojnacka-Wójcik, E
Bojarski, AJ
机构：
[1] Polish Acad Sci, Inst Pharmacol, Dept Med Chem, PL-31343 Krakow, Poland
[2] Polish Acad Sci, Inst Pharmacol, Dept New Drug Res, PL-31343 Krakow, Poland
[3] Jagiellonian Univ, Coll Med, Dept Pharmaceut Chem, PL-30688 Krakow, Poland
来源：
POLISH JOURNAL OF PHARMACOLOGY | 2001年 / 53卷 / 04期
关键词：
1-arylpiperazine derivatives; 3-propyl-beta-tetralonohydantoins; 5-HT1A and 5-HT2A receptor affinity; structure-activity relationship;
D O I：
暂无
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
A series of new analogues of 3-[3-(4-arylpiperazinyl)-propyl]-cyclohexane-1',5-spirohydantoin (2), with aromatic ring fused in amide moiety (4-9) were synthesized and evaluated for affinity at 5-HT1A and 5-HT2A receptors. The influence of the substitution mode in the phenyl ring of phenylpiperazine moiety on the affinity for both receptors has been discussed. The most potent 5-HT1A (9, K-i = 53 nM) and 5-HT2A (4, 6, 8 and 9; K-i = 14-76 nM) ligands were evaluated in in vivo tests. The obtained results indicate that all in vivo tested compounds showed pharmacological profile of 5-HT2A antagonists. Additionally, a m-CF3 derivative (9), behaved like a partial agonist (agonist of pre- and antagonist of postsynaptic) of 5-HT1A receptors and may offer a new lead for the development of potential psychotropic agents.
引用
收藏
页码：395 / 401
页数：7
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