Serotonin receptor physiology : Relation to emesis

• Published in: Digestive diseases and sciences Vol. 44; no. 8; pp. 108S - 113S
• Main Author: HASLER, W. L
• Format: Conference Proceeding Journal Article
• Language: English
• Published: Heidelberg Springer 01.08.1999
• Subjects: Adolescent; Adult; Analytical, structural and metabolic biochemistry; Biological and medical sciences; Central Nervous System - drug effects; Central Nervous System - physiopathology; Child; Child, Preschool; Enteric Nervous System - drug effects; Enteric Nervous System - physiopathology; Female; Fundamental and applied biological sciences. Psychology; Humans; Infant; Male; Non peptidic neurotransmitters, polyamines; Other biological molecules; Periodicity; Receptors, Serotonin - classification; Receptors, Serotonin - drug effects; Receptors, Serotonin - physiology; Serotonin Agents - adverse effects; Serotonin Agents - therapeutic use; Syndrome; Vomiting - drug therapy; Vomiting - physiopathology; Human; Signal transduction; Molecular form; Ligand; Vomiting; Digestive diseases; Review; Serotonine receptor; Molecular biology; Biological activity
• ISSN: 0163-2116

Several serotonin (5-HT) receptor subtypes have been defined by pharmacological responses to selective agonists and antagonists and by pathways of receptor-effector coupling. Using molecular techniques, additional receptor subtypes have been described. 5-HT receptors are prevalent in the central nervous system and gut and participate in induction of emesis. 5-HT3 antagonists are used to prevent emesis from cancer chemotherapy and also demonstrate efficacy in radiation-induced nausea, postoperative nausea, hyperemesis gravidarum, and nausea and vomiting with the acquired immunodeficiency syndrome. 5-HT4 agonists exhibit prokinetic properties in nauseated patients with gastroparesis and functional dyspepsia. Conversely, 5-HT4 antagonists have antiemetic activity in some experimental models. The 5-HT1D receptor agonist sumatriptan reduces emesis with migraine headaches and in cyclic vomiting syndrome, most likely via action on central nervous system sites. In other models, 5-HT1A and 5-HT2A/5-HT2C agonists exhibit antiemetic properties. The utility of 5-HT receptor ligands in treating emesis is the subject of active investigation.