title: Synthesis and structure-activity relationship of 2-(aminoalkyl)-3,3a,8,12b-tetrahydro-2H-dibenzocyclohepta[1,2-b]furan derivatives: a novel series of 5-HT(2A/2C) receptor antagonists.
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 a series of substituted 2-(aminomethyl)-3,3a,8,12b-tetrahydro-2H-dibenzocyclohepta[1,2-b]furan derivatives. The 5-HT2A, 5-HT2C and H1 receptor affinities of the described compounds are reported. The mCCP antagonistic activity of a set of selected molecules is also reported.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development, a division of Janssen-Cilag, Medicinal Chemistry Department, Jarama s/n, 45007 Toledo, Spain. jcid@prdes.jnj.com
authors.forename: José
authors.initials: J
authors.lastname: Cid
authors.forename: José M
authors.initials: JM
authors.lastname: Alonso
authors.forename: José I
authors.initials: JI
authors.lastname: Andrés
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
authors.forename: Andrés A
authors.initials: AA
authors.lastname: Trabanco
mesh_terms: D005663:Furans / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D008024:Ligands; D011485:Protein Binding; D011869:Radioligand Assay; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D005663:Furans; D008024:Ligands; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists