title: Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.
abstract: The synthesis of a series of novel 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives as well as their 5-HT(2A/2C) and H(1) receptor binding affinities are described. The in vivo activity as potential anxiolytics of the synthesised compounds was measured in a mCPP challenge test. One of the compounds, 2a, proved to be a potent 5-HT(2A/2C) receptor antagonist showing as well oral activity and therefore could be considered as a potential anxiolytic/antidepressant agent.
authors.affiliation: Janssen-Cilag, Basic Research Centre, Jarama s/n, 45007 Toledo, Spain. jandres@jaces.jnj.com
authors.forename: J Ignacio
authors.initials: JI
authors.lastname: Andrés
authors.forename: Jesús
authors.initials: J
authors.lastname: Alcázar
authors.forename: José M
authors.initials: JM
authors.lastname: Alonso
authors.forename: Adolfo
authors.initials: A
authors.lastname: Díaz
authors.forename: Javier
authors.initials: J
authors.lastname: Fernández
authors.forename: Pilar
authors.initials: P
authors.lastname: Gil
authors.forename: Laura
authors.initials: L
authors.lastname: Iturrino
authors.forename: Encarna
authors.initials: E
authors.lastname: Matesanz
authors.forename: Theo F
authors.initials: TF
authors.lastname: Meert
authors.forename: Anton
authors.initials: A
authors.lastname: Megens
authors.forename: Victor K
authors.initials: VK
authors.lastname: Sipido
mesh_terms: D000818:Animals; D001381:Azepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016466:CHO Cells; D006224:Cricetinae; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D044402:Receptor, Serotonin, 5-HT2A; D044405:Receptor, Serotonin, 5-HT2C; D011985:Receptors, Serotonin / Q000187:drug effects*; D012702:Serotonin Antagonists / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D001381:Azepines; D044402:Receptor, Serotonin, 5-HT2A; D044405:Receptor, Serotonin, 5-HT2C; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists