Serotonin Receptor and Transporter Ligands - Current Status

Author(s): Seung Jun Oh, Hyun-Joon Ha, Dae Yoon Chi, Hee Kyung Lee

Journal Name: Current Medicinal Chemistry

Volume 8 , Issue 9 , 2001

Become EABM
Become Reviewer
Call for Editor


The serotonin (5-HT) receptor system has 14 different subtypes classified by pharmacology and function. Many ligands are widely used for therapeutic and diagnostic purposes in some severe human diseases. Most of the ligands that are specific for each 5-HT receptor have distinctive chemical structures with regard to pharmacophore elements including 4-arylpiperazine, benzimidazole, benzamide, chroman, aminopyridazine, tetralin, and polycycles. However, their affinity and selectivity for 5-HT, dopamine and a1 receptors depend on their substituents and linker spacers. 5-HT transporter inhibitors have also been developed as potential antidepressants. In contrast to classical tricyclic compounds, newly developed secondary amine derivatives such as paroxetine and tetralin show high binding affinity and selectivity. Radioisotope-labeled ligands have also been developed, including [carbonyl-11 C]WAY 100635 for 5-HT1A receptor, [ 11 C or 18 F]ketanserine derivatives for 5-HT2 receptor, [ 125 I]DAIZAC for 5-HT3 receptor, and [ 123 I]IDAM for 5-HT transporter, and these are accumulated in brain regions that are rich in the respective receptors. This review summarizes the recent development of 5-HT receptor- and transporter-specific ligands and their pharmacological properties on the basis of their chemical structures.

Keywords: Transporter Ligands, serotonin HT, antidepepressants, G-protein ion channel, central nervous system cns, ht receptor ligands, Zacopride, Metoci opramide, Ondansetron, Indolyloxadiazole

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2001
Page: [999 - 1034]
Pages: 36
DOI: 10.2174/0929867013372599
Price: $65

Article Metrics

PDF: 8