Background: Serotonin is an important biogenic amine and is implicated in wideranging physiological and physiopathological processes. Pharmacological manipulation of the serotoninergic system is believed to have a great therapeutic potential.

Objectives: In order to identify selective ligands for 5-HT1A, 5-HT2A and 5-HT2C receptors two series of 4-substituted piperazine derivatives, bearing indolic or methyl indolic nuclei, were synthesized.

Methods: All the compounds, synthesized by standard solution methods, were evaluated for 5- HT1A, 5-HT2A and 5-HT2C receptors. The highest affine and selective compounds have been evaluated also on dopaminergic (D1 and D2) and adrenergic (α1A and α2A) receptors.

Results: Several of the newly synthesized molecules showed affinity in the nanomolar range for 5- HT1A, 5-HT2A and 5-HT2C receptors and moderate to no affinity for other relevant receptors (D1, D2, α1A and α2A).

Conclusion: Compounds 7f and 10a showed a nanomolar affinity towards 5-HT1A with an in vitro pharmacologic profile compatible with antipsychotic drugs.

背景：5-羟色胺是一种重要的生物胺，与广泛的生理和生理病理过程有关。血清素能系统的药理学操作被认为具有巨大的治疗潜力。

目的：为了鉴定5-HT1A，5-HT2A和5-HT2C受体的选择性配体，合成了两个带有吲哚或甲基吲哚核的4-取代哌嗪衍生物系列。

方法：通过标准溶液法合成的所有化合物均经过5-HT1A，5-HT2A和5-HT2C受体评估。对多巴胺能受体（D1和D2）和肾上腺素能受体（α1A和α2A）也评估了最高的仿射和选择性化合物。

结果：一些新合成的分子显示出对5-HT1A，5-HT2A和5-HT2C受体的亲和力在纳摩尔范围内，对其他相关受体（D1，D2，α1A和α2A）的亲和力中等至无。

结论：化合物7f和10a对5-HT1A具有纳摩尔摩尔亲和力，其体外药理学特征与抗精神病药兼容。