5-HT3 Receptors as Targets for Biologically Active Compounds (Review)

Subtype 3 serotonin receptors (5-HT3 receptors) are members of the cis-loop ligand-dependent ion channel family and have been studied intensely during the last 40 years. The structure of the main prototype, i.e., the homomeric 3A receptor, has now been determined; evidence of the existence and functional activity of heteromeric versions has been obtained. A multitude of ligands of 5-HT3 receptors has been studied and described, and these investigations continue as these compounds have great pharmaceutical potential. Along with the current use of 5-HT3 antagonists in a number of pathological states, including nausea and vomiting of various etiologies and irritable bowel syndrome, the evidence base for the potential of these compounds for other indications is growing quickly, especially in relation to anxiolytic, antipsychotic, and analgesic effects, as well as for the effective correction of alcohol addiction and inflammatory reactions. This review provides a brief description of the structural-functional characteristics of 5-HT3 receptors and their ligands, and the most important potentials for their use in clinical and experimental pharmacology are discussed.