Serotonin is a neuromediator well known for its implication in mood regulation, anxiety, depression,insomnia as well as in normal human function such as sleep, sexual activity and appetite and recently it was demonstrated its involvement in the proliferation of human tumor cells. In this way serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists and pharmaceutical companies. Among 5-HTRs, the5-HT1A subtype is the best studied and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind 5-HT1A receptor sites such as aminotetralins, ergolines, arylpiperazines, indolylalkylamines, aporphines and aryloxyalkilamines. In this manuscript, we report an overview regarding some of the arylpiperazine derivatives that we have synthesized as 5-HT1A receptor ligands, characterized with the introduction of different heterocyclic nuclei.