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间隔结构对长链芳基哌嗪配体组中5-HT7和5-HT1A受体亲和力的影响。

The impact of spacer structure on 5-HT7 and 5-HT1A receptor affinity in the group of long-chain arylpiperazine ligands.

作者信息

Bojarski Andrzej J, Duszyńska Beata, Kołaczkowski Marcin, Kowalski Piotr, Kowalska Teresa

机构信息

Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31-343 Kraków, Poland.

出版信息

Bioorg Med Chem Lett. 2004 Dec 6;14(23):5863-6. doi: 10.1016/j.bmcl.2004.09.029.

DOI:10.1016/j.bmcl.2004.09.029
PMID:15501057
Abstract

New cis-, trans-2-butene and 1,2-bismethylbenzene analogues of MM77 and NAN-190 (1-[4-[4-(2-methoxyphenyl)-piperazin-1-yl]-butyl]-pyrrolidine-2,5-dione and isoindole-1,3-dione, respectively) were synthesized. The differences in their in vitro affinity for serotonin 5-HT(7) and 5-HT(1A) receptors were explained using a conformational analysis. A bioactive conformation of those compounds for the 5-HT(7) receptor, different from that established for 5-HT(1A), was proposed.

摘要

合成了MM77和NAN - 190（分别为1 - [4 - [4 - (2 - 甲氧基苯基)-哌嗪 - 1 - 基]-丁基]-吡咯烷 - 2,5 - 二酮和异吲哚 - 1,3 - 二酮）的新顺式、反式 - 2 - 丁烯和1,2 - 二甲基苯类似物。利用构象分析解释了它们对5 - 羟色胺5 - HT(7)和5 - HT(1A)受体的体外亲和力差异。提出了这些化合物针对5 - HT(7)受体的生物活性构象，该构象不同于针对5 - HT(1A)所确定的构象。

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