title: Controversies on the role of 5-HT(2C) receptors in the mechanisms of action of antidepressant drugs.
abstract: Evidence from the various sources indicates alterations in 5-HT2C receptor functions in anxiety, depression and suicide, and other stress-related disorders treated with antidepressant drugs. Although the notion of a 5-HT2C receptor desensitization following antidepressant treatments is rather well anchored in the literature, this concept is mainly based on in vitro assays and/or behavioral assays (hypolocomotion, hyperthermia) that have poor relevance to anxio-depressive disorders. Our objective herein is to provide a comprehensive overview of the studies that have assessed the effects of antidepressant drugs on 5-HT2C receptors. Relevant molecular (second messengers, editing), neurochemical (receptor binding and mRNA levels), physiological (5-HT2C receptor-induced hyperthermia and hormone release), behavioral (5-HT2C receptor-induced changes in feeding, anxiety, defense and motor activity) data are summarized and discussed. Setting the record straight about drug-induced changes in 5-HT2C receptor function in specific brain regions should help to determine which pharmacotherapeutic strategy is best for affective and anxiety disorders.
authors.affiliation: INSERM UMR S894, Centre de Psychiatrie et Neurosciences, Paris, France; UPMC, Univ Paris 06, Paris, France; Paris Descartes, Univ Paris 05, Paris, France.
authors.forename: Cedric B P
authors.initials: CB
authors.lastname: Martin
authors.affiliation: INSERM UMR S894, Centre de Psychiatrie et Neurosciences, Paris, France; UPMC, Univ Paris 06, Paris, France; Paris Descartes, Univ Paris 05, Paris, France.
authors.forename: Michel
authors.initials: M
authors.lastname: Hamon
authors.affiliation: INSERM UMR S894, Centre de Psychiatrie et Neurosciences, Paris, France; UPMC, Univ Paris 06, Paris, France; Paris Descartes, Univ Paris 05, Paris, France.
authors.forename: Laurence
authors.initials: L
authors.lastname: Lanfumey
authors.affiliation: INSERM UMR S894, Centre de Psychiatrie et Neurosciences, Paris, France; Paris Descartes, Univ Paris 05, Paris, France; EA4475 - Pharmacologie de la circulation cérébrale, Paris, France. Electronic address: raymond.mongeau@parisdescartes.fr.
authors.forename: Raymond
authors.initials: R
authors.lastname: Mongeau
mesh_terms: D000818:Animals; D000928:Antidepressive Agents / Q000494:pharmacology*; D001007:Anxiety / Q000188:drug therapy / Q000503:physiopathology; D001921:Brain / Q000187:drug effects / Q000503:physiopathology; D003866:Depressive Disorder / Q000188:drug therapy / Q000503:physiopathology; D006801:Humans; D044405:Receptor, Serotonin, 5-HT2C / Q000378:metabolism*; D013315:Stress, Psychological / Q000188:drug therapy / Q000503:physiopathology
chemical_list: D000928:Antidepressive Agents; D044405:Receptor, Serotonin, 5-HT2C
keywords: 5-HTT; Anxiety; Depression; Editing; SSRI; Serotonin(2C); Splicing