López-Rodríguez M L, Morcillo M J, Fernández E, Porras E, Murcia M, Sanz A M, Orensanz L
Departamento de Química Orgánica I, Facultad de Ciencias Químicas, Universidad Complutense, Madrid, Spain.
J Med Chem. 1997 Aug 1;40(16):2653-6. doi: 10.1021/jm970216k.
A series of new arylpiperazine derivatives 2, which are devoid of the terminal amide fragment present in related 5-HT1A ligands, was prepared and evaluated for affinity at 5-HT1A and alpha 1 receptors. All the compounds 2 demonstrated high affinity for the 5-HT1A receptor and moderate affinity for alpha 1 receptor binding sites. Structure-activity relationship (SAR) studies suggest that there is influence of electronic factors on the no-pharmacophoric part of the alpha 1 receptor site. However there is no influence of electronic interactions on the stabilization of the 5-HT1A receptor-ligand complex.
制备了一系列新的芳基哌嗪衍生物2，这些衍生物没有相关5-HT1A配体中存在的末端酰胺片段，并对其与5-HT1A和α1受体的亲和力进行了评估。所有化合物2对5-HT1A受体表现出高亲和力，对α1受体结合位点表现出中等亲和力。构效关系（SAR）研究表明，电子因素对α1受体位点的非药效基团部分有影响。然而，电子相互作用对5-HT1A受体-配体复合物的稳定性没有影响。
