Serotonin receptor physiology: relation to emesis.
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.
Hasler
W L
WL
Department of Internal Medicine, University of Michigan, Ann Arbor 48109, USA.
D000293:Adolescent; D000328:Adult; D002490:Central Nervous System / Q000187:drug effects / Q000503:physiopathology; D002648:Child; D002675:Child, Preschool; D017615:Enteric Nervous System / Q000187:drug effects / Q000503:physiopathology; D005260:Female; D006801:Humans; D007223:Infant; D008297:Male; D010507:Periodicity; D011985:Receptors, Serotonin / Q000145:classification / Q000187:drug effects / Q000502:physiology*; D018490:Serotonin Agents / Q000009:adverse effects / Q000627:therapeutic use; D013577:Syndrome; D014839:Vomiting / Q000188:drug therapy / Q000503:physiopathology*
D011985:Receptors, Serotonin; D018490:Serotonin Agents