3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor

J Med Chem. 1994 May 13;37(10):1402-5. doi: 10.1021/jm00036a002.

Authors

J J Kulagowski¹, R Baker, N R Curtis, P D Leeson, I M Mawer, A M Moseley, M P Ridgill, M Rowley, I Stansfield, A C Foster, et al.

Affiliation

¹ Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Harlow, Essex, U.K.

PMID: 8182696
DOI: 10.1021/jm00036a002

No abstract available

MeSH terms

Administration, Oral
Aminoquinolines / metabolism
Animals
Anticonvulsants / pharmacology
Binding Sites / drug effects
Binding, Competitive
Blood-Brain Barrier
Brain / metabolism
Glycine / antagonists & inhibitors*
Hydroxyquinolines / chemical synthesis
Hydroxyquinolines / metabolism
Hydroxyquinolines / pharmacology*
In Vitro Techniques
Mice
Mice, Inbred DBA
Rats
Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
Receptors, N-Methyl-D-Aspartate / metabolism
Structure-Activity Relationship

Substances

Aminoquinolines
Anticonvulsants
Hydroxyquinolines
Receptors, N-Methyl-D-Aspartate
4-trans-2-carboxy-5,7-dichloro-4-phenylaminocarbonylamino-1,2,3,4-tetrahydroquinoline
Glycine