title: 2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties.
abstract: Following the program started at Johnson & Johnson Pharmaceutical Research & Development searching for 5-HT(2A/2C) antagonists, we now report on the synthesis of 2-(dimethylaminomethyl)-2,3,3a,8-tetrahydroisoxazolo[3,2-a]pyrido[3,4-c]-[2]benzazepine and 2-(dimethylaminomethyl)-2,3,3a,8-tetrahydroisoxazolo[3,2-a]pyrido[3,2-c]-[2]benzazepine. A new method for the synthesis of pyridobenzazepines is described as well. The affinities for several receptors as well as the mCPP antagonistic activity of the compounds synthesised are described.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development, Division of Janssen-Cilag, Medicinal Chemistry Department, Jarama s/n, 45007 Toledo, Spain. iandres@prdes.jnj.com
authors.forename: J Ignacio
authors.initials: JI
authors.lastname: Andrés
authors.forename: José M
authors.initials: JM
authors.lastname: Alonso
authors.forename: Javier
authors.initials: J
authors.lastname: Fernández
authors.forename: Laura
authors.initials: L
authors.lastname: Iturrino
authors.forename: Pedro
authors.initials: P
authors.lastname: Martínez
authors.forename: Theo F
authors.initials: TF
authors.lastname: Meert
authors.forename: Victor K
authors.initials: VK
authors.lastname: Sipido
mesh_terms: D000818:Animals; D014151:Anti-Anxiety Agents / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D001552:Benzazepines / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D003500:Cyclization; D006801:Humans; D007279:Injections, Subcutaneous; D008297:Male; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D044402:Receptor, Serotonin, 5-HT2A; D044405:Receptor, Serotonin, 5-HT2C; D011969:Receptors, Histamine H1 / Q000187:drug effects; D011985:Receptors, Serotonin / Q000187:drug effects*; D012702:Serotonin Antagonists / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D014151:Anti-Anxiety Agents; D001552:Benzazepines; D044402:Receptor, Serotonin, 5-HT2A; D044405:Receptor, Serotonin, 5-HT2C; D011969:Receptors, Histamine H1; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists