title: [3H]-(R)-NPTS, a radioligand for the type 1 glycine transporter.
abstract: The synthesis of NPTS, 6, a potent inhibitor of the type 1 glycine transporter (GlyT1) is described, as well as preparation of 6 in optically active and tritiated form for use as a radioligand for affinity displacement assay of GlyT1.
authors.affiliation: Central Research Division, Pfizer Inc., Groton, CT 06340, USA. john_a_lowe@groton.pfizer.com
authors.forename: John A
authors.initials: JA
authors.lastname: Lowe
authors.forename: Susan E
authors.initials: SE
authors.lastname: Drozda
authors.forename: Katherine
authors.initials: K
authors.lastname: Fisher
authors.forename: Christine
authors.initials: C
authors.lastname: Strick
authors.forename: Lorraine
authors.initials: L
authors.lastname: Lebel
authors.forename: Christopher
authors.initials: C
authors.lastname: Schmidt
authors.forename: Donna
authors.initials: D
authors.lastname: Hiller
authors.forename: Kathleen S
authors.initials: KS
authors.lastname: Zandi
mesh_terms: D026921:Amino Acid Transport Systems, Neutral / Q000037:antagonists & inhibitors*; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D050487:Glycine Plasma Membrane Transport Proteins; D006624:Hippocampus / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D012521:Sarcosine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D013237:Stereoisomerism; D009435:Synaptic Transmission / Q000187:drug effects; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism; D014407:Tumor Cells, Cultured
chemical_list: C478321:(R)-N(3-phenyl-3-(4'-(4-toluoyl)phenoxy)-propyl)sarcosine; D026921:Amino Acid Transport Systems, Neutral; D050487:Glycine Plasma Membrane Transport Proteins; D019275:Radiopharmaceuticals; C493268:SLC6A9 protein, human; C493266:Slc6a9 protein, rat; D012521:Sarcosine