title: Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists.
abstract: The understanding of the physiological role of the G-protein coupled serotonin 5-HT(7) receptor is largely rudimentary. Therefore, selective and potent pharmacological tools will add to the understanding of serotonergic effects mediated through this receptor. In this report, we describe two compound classes, chromans and tetralins, encompassing compounds with nanomolar affinity for the 5-HT(7) receptor and with good selectivity. Within theses classes, we have discovered both agonists and antagonists that can be used for further understanding of the pharmacology of the 5-HT(7) receptor.
authors.affiliation: Organic Pharmaceutical Chemistry, Uppsala University, Uppsala Biomedical Centre, Box 574, SE-751 23 Uppsala, Sweden.
authors.forename: Pär
authors.initials: P
authors.lastname: Holmberg
authors.forename: Daniel
authors.initials: D
authors.lastname: Sohn
authors.forename: Robert
authors.initials: R
authors.lastname: Leideborg
authors.forename: Patrizia
authors.initials: P
authors.lastname: Caldirola
authors.forename: Pavel
authors.initials: P
authors.lastname: Zlatoidsky
authors.forename: Sverker
authors.initials: S
authors.lastname: Hanson
authors.forename: Nina
authors.initials: N
authors.lastname: Mohell
authors.forename: Susanne
authors.initials: S
authors.lastname: Rosqvist
authors.forename: Gunnar
authors.initials: G
authors.lastname: Nordvall
authors.forename: Anette M
authors.initials: AM
authors.lastname: Johansson
authors.forename: Rolf
authors.initials: R
authors.lastname: Johansson
mesh_terms: D000818:Animals; D016466:CHO Cells; D002839:Chromans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006224:Cricetinae; D000242:Cyclic AMP / Q000096:biosynthesis; D008024:Ligands; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000378:metabolism; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017366:Serotonin Receptor Agonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D002839:Chromans; D008024:Ligands; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists; D013764:Tetrahydronaphthalenes; C104425:serotonin 7 receptor; D000242:Cyclic AMP