Novel Selective Arylpiperazine Ligands for the Serotonin 5-HT1a Receptor

被引：0
|
作者：
Romeo, G. [1 ]
机构：
[1] Univ Catania, Dipartimento Sci Farmaceut, I-95125 Catania, Italy
来源：
JOINT MEETING ON MEDICAL CHEMISTRY | 2009年
关键词：
DERIVATIVES; ANTAGONIST; LECOZOTAN; POTENT; MEMORY;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Among the several serotonin membrane receptors, 5-HT(1A)R is one of the most studied. Owing to its widespread presence in CNS and its involvement in a number of diseases, such as anxiety and depression, and cognitive processes, such as learning and memory, 5-HT(1A)R represents a potential target for therapeutically effective drugs. Over the years, our research group has been involved in the design of arylpiperazine compounds as selective 5-HT(1A)R ligands. Here we discuss some recent results in this field and the discovery of 2-[[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]thio]benzoxazole, an antagonist which displays very high affinity (K(i) = 0.094 nM) and selectivity for 5-HT(1A)R. over many other related receptors.
引用
收藏
页码：15 / 19
页数：5
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