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4-[2-(3-甲氧基苯基)乙基]-1-(2-甲氧基苯基)哌嗪的二价配体方法：5-HT(7)和5-HT(1A)受体的合成及结合亲和力

Bivalent ligand approach on 4-[2-(3-methoxyphenyl)ethyl]-1-(2-methoxyphenyl)piperazine: synthesis and binding affinities for 5-HT(7) and 5-HT(1A) receptors.

作者信息

Leopoldo Marcello, Lacivita Enza, Colabufo Nicola A, Niso Mauro, Berardi Francesco, Perrone Roberto

机构信息

Università degli Studi di Bari, Dipartimento Farmaco-Chimico, via Orabona, 4, Bari, Italy.

出版信息

Bioorg Med Chem. 2007 Aug 1;15(15):5316-21. doi: 10.1016/j.bmc.2007.05.010. Epub 2007 May 6.

DOI:10.1016/j.bmc.2007.05.010
PMID:17517509
Abstract

We here report on the synthesis and binding properties at 5-HT(7) and 5-HT(1A) receptors of ligands 3-12, that were designed according to the 'bivalent ligand' approach. Two moieties of the 5-HT(7)/5-HT(1A) ligand 4-[2-(3-methoxyphenyl)ethyl]-1-(2-methoxyphenyl)piperazine (1) were linked through their 3-methoxy substituent by polymethylene chains of variable length, with the aim to increase the affinity for 5-HT(7) receptor and the selectivity over 5-HT(1A) receptors. In the best cases, the dimers showed affinities for 5-HT(7) receptors as high as the monomer with no improvement in selectivity. Some dimers displayed 5-HT(1A) receptor affinities slightly higher than monomer 1.

摘要

我们在此报告根据“二价配体”方法设计的配体3 - 12在5 - HT(7)和5 - HT(1A)受体上的合成及结合特性。5 - HT(7)/5 - HT(1A)配体4 - [2 - (3 - 甲氧基苯基)乙基] - 1 - (2 - 甲氧基苯基)哌嗪(1)的两个部分通过不同长度的亚甲基链经其3 - 甲氧基取代基相连，目的是提高对5 - HT(7)受体的亲和力以及对5 - HT(1A)受体的选择性。在最佳情况下，二聚体对5 - HT(7)受体的亲和力与单体一样高，但选择性没有提高。一些二聚体对5 - HT(1A)受体的亲和力略高于单体1。

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