Derivatives as 5HT1A Receptor Ligands-Past and Present

G.      Caliendo; V.      Santagada; E.      Perissutti; F.      Fiorino

doi:10.2174/0929867054367220

Abstract

Serotonin is a neuromediator, well-know for its implication in mood regulation, anxiety, depression and, insomnia as well as in normal human function such as sleep, sexual activity and appetite. In this way, serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists and pharmaceutical companies. Among 5-HTRs, the 5-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 aryloxyalkyl-amines.

Keywords: serotonin, neurotransmitter, g protein-coupled receptors, median raphe nucleus (mrn), ohdpat, enantioselectivity, indolylalkylamines, ergolines, aporphines, qsar