Discovery and SAR of org 24598-a selective glycine uptake inhibitor.
The discovery of Org 24598, one of the first potent and selective inhibitors of the glycine transporter is discussed. In vitro structure-activity relationships (SARs) data for interaction of a ligand with this system is discussed.
Brown
A
A
Department of Medicinal Chemistry, Organon Research and Development Group, Newhouse, Lanarkshire ML1 5SH, Scotland, UK.
Carlyle
I
I
Clark
J
J
Hamilton
W
W
Gibson
S
S
McGarry
G
G
McEachen
S
S
Rae
D
D
Thorn
S
S
Walker
G
G
D026921:Amino Acid Transport Systems, Neutral; D000818:Animals; D001921:Brain / Q000378:metabolism; D002352:Carrier Proteins / Q000037:antagonists & inhibitors* / Q000187:drug effects*; D050485:GABA Plasma Membrane Transport Proteins; D005998:Glycine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D050487:Glycine Plasma Membrane Transport Proteins; D008565:Membrane Proteins / Q000187:drug effects; D026901:Membrane Transport Proteins; D050484:Norepinephrine Plasma Membrane Transport Proteins; D027361:Organic Anion Transporters; D011869:Radioligand Assay; D051381:Rats; D018009:Receptors, Glycine; D016194:Receptors, N-Methyl-D-Aspartate / Q000819:agonists*; D012680:Sensitivity and Specificity; D013131:Spine / Q000378:metabolism; D013329:Structure-Activity Relationship; D027981:Symporters
D026921:Amino Acid Transport Systems, Neutral; D002352:Carrier Proteins; D050485:GABA Plasma Membrane Transport Proteins; D050487:Glycine Plasma Membrane Transport Proteins; D008565:Membrane Proteins; D026901:Membrane Transport Proteins; D050484:Norepinephrine Plasma Membrane Transport Proteins; D027361:Organic Anion Transporters; D018009:Receptors, Glycine; D016194:Receptors, N-Methyl-D-Aspartate; C493226:Slc6a2 protein, rat; D027981:Symporters; C435781:org 24598; D005998:Glycine