title: Discovery and SAR studies of novel GlyT1 inhibitors.
abstract: Inhibition of the glycine transporter GlyT1 is a potential strategy for the treatment of schizophrenia. A novel series of GlyT1 inhibitors and their structure-activity relationships (SAR) are described. Members of this series are highly potent and selective transport inhibitors which are shown to elevate glycine levels in cerebrospinal fluid.
authors.affiliation: Lilly Research Laboratories, Eli Lilly and Company, Erl Wood Manor, Windlesham, Surrey GU20 6PH, UK. magnus.walter@lilly.com
authors.forename: Magnus W
authors.initials: MW
authors.lastname: Walter
authors.forename: Beth J
authors.initials: BJ
authors.lastname: Hoffman
authors.forename: Kimberly
authors.initials: K
authors.lastname: Gordon
authors.forename: Kirk
authors.initials: K
authors.lastname: Johnson
authors.forename: Patrick
authors.initials: P
authors.lastname: Love
authors.forename: Matthew
authors.initials: M
authors.lastname: Jones
authors.forename: Teresa
authors.initials: T
authors.lastname: Man
authors.forename: Lee
authors.initials: L
authors.lastname: Phebus
authors.forename: Jon K
authors.initials: JK
authors.lastname: Reel
authors.forename: Helene C
authors.initials: HC
authors.lastname: Rudyk
authors.forename: Harlan
authors.initials: H
authors.lastname: Shannon
authors.forename: Kjell
authors.initials: K
authors.lastname: Svensson
authors.forename: Hong
authors.initials: H
authors.lastname: Yu
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Valli
authors.forename: Warren J
authors.initials: WJ
authors.lastname: Porter
mesh_terms: D000818:Animals; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D050487:Glycine Plasma Membrane Transport Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D050487:Glycine Plasma Membrane Transport Proteins; C493266:Slc6a9 protein, rat