title: Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety.
abstract: A series of nortropane analogs based on previously reported compound 1 have been synthesized and shown to bind to the nociceptin receptor with high affinity. The synthesis and structure-activity relationships around the C-3 nortropane substitution are described. From the SAR study and hPXR screening effort, compound 15 was identified to possess potent oral antitussive and anxiolytic-like activities in the guinea pig models.
authors.affiliation: Department of Chemical Research-CV & CNS, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
authors.forename: Shu-Wei
authors.initials: SW
authors.lastname: Yang
authors.forename: Ginny
authors.initials: G
authors.lastname: Ho
authors.forename: Deen
authors.initials: D
authors.lastname: Tulshian
authors.forename: William J
authors.initials: WJ
authors.lastname: Greenlee
authors.forename: Zheng
authors.initials: Z
authors.lastname: Tan
authors.forename: Hongtao
authors.initials: H
authors.lastname: Zhang
authors.forename: April
authors.initials: A
authors.lastname: Smith-Torhan
authors.forename: Ahmad
authors.initials: A
authors.lastname: Fawzi
authors.forename: John
authors.initials: J
authors.lastname: Anthes
authors.forename: Sherry
authors.initials: S
authors.lastname: Lu
authors.forename: Geoffrey
authors.initials: G
authors.lastname: Varty
authors.forename: Xiomara
authors.initials: X
authors.lastname: Fernandez
authors.forename: Robbie L
authors.initials: RL
authors.lastname: McLeod
authors.forename: John
authors.initials: J
authors.lastname: Hey