title: Discovery of a novel non-steroidal GR antagonist with in vivo efficacy in the olanzapine-induced weight gain model in the rat.
abstract: We report the optimization of a series of non-steroidal GR antagonists that led to the identification of compound 7. This compound is efficacious when dosed orally in an olanzapine-induced weight gain model in rats.
authors.affiliation: Corcept Therapeutics, 149 Commonwealth Drive, Menlo Park, CA 94025, USA. hhunt@corcept.com
authors.forename: Hazel J
authors.initials: HJ
authors.lastname: Hunt
authors.forename: Nicholas C
authors.initials: NC
authors.lastname: Ray
authors.forename: George
authors.initials: G
authors.lastname: Hynd
authors.forename: Jon
authors.initials: J
authors.lastname: Sutton
authors.forename: Mohammed
authors.initials: M
authors.lastname: Sajad
authors.forename: Elizabeth
authors.initials: E
authors.lastname: O'Connor
authors.forename: Shahadat
authors.initials: S
authors.lastname: Ahmed
authors.forename: Peter
authors.initials: P
authors.lastname: Lockey
authors.forename: Steve
authors.initials: S
authors.lastname: Daly
authors.forename: Gerry
authors.initials: G
authors.lastname: Buckley
authors.forename: Robin D
authors.initials: RD
authors.lastname: Clark
authors.forename: Robert
authors.initials: R
authors.lastname: Roe
authors.forename: Christine
authors.initials: C
authors.lastname: Blasey
authors.forename: Joe
authors.initials: J
authors.lastname: Belanoff
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001569:Benzodiazepines / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D023421:Models, Animal; D015394:Molecular Structure; D000077152:Olanzapine; D051381:Rats; D017207:Rats, Sprague-Dawley; D011965:Receptors, Glucocorticoid / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013941:Thymine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D015430:Weight Gain / Q000187:drug effects*
chemical_list: C000606526:CORT118335; D011965:Receptors, Glucocorticoid; D001569:Benzodiazepines; D000077152:Olanzapine; D013941:Thymine