Derivatives as 5HT1A Receptor Ligands-Past and Present

Authors: Caliendo, G.; Santagada, V.; Perissutti, E.; Fiorino, F.

Source: Current Medicinal Chemistry, Volume 12, Number 15, July 2005 , pp. 1721-1753(33)

Publisher: Bentham Science Publishers

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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

Document Type: Review article

DOI: http://dx.doi.org/10.2174/0929867054367220

Affiliations: 1: Dipartimento di Chimica Farmaceutica e Tossicologica, Via D. Montesano, 49, 80131 Naples, Italy.

Publication date: 2005-07-01

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Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.