[3H]-(R)-NPTS, a radioligand for the type 1 glycine transporter.
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.
Lowe
John A
JA
Central Research Division, Pfizer Inc., Groton, CT 06340, USA. john_a_lowe@groton.pfizer.com
Drozda
Susan E
SE
Fisher
Katherine
K
Strick
Christine
C
Lebel
Lorraine
L
Schmidt
Christopher
C
Hiller
Donna
D
Zandi
Kathleen S
KS
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
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