NPS 1506, a moderate affinity uncompetitive NMDA receptor antagonist: preclinical summary and clinical experience.
NPS Pharmaceuticals, Inc. (NPS) has synthesized a series of open-channel blockers with varying potencies at the NMDA receptor. NPS 1506 (Fig. 1) is a moderate affinity antagonist that inhibits NMDA/glycine-induced increases in cytosolic calcium in cultured rat cerebellar granule cells (IC50 = 476nM) and displaces the binding of [3H]MK-801 to rat cortical membranes (IC50 = 664nM).
Mueller
A L
AL
NPS Pharmaceuticals, Inc., Salt Lake City, Utah 84108, USA.
Artman
L D
LD
Balandrin
M F
MF
Brady
E
E
Chien
Y
Y
DelMar
E G
EG
Kierstead
A
A
Marriott
T B
TB
Moe
S T
ST
Raszkiewicz
J L
JL
VanWagenen
B
B
Wells
D
D
D000293:Adolescent; D000328:Adult; D000818:Animals; D002478:Cells, Cultured; D002540:Cerebral Cortex / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D016291:Dizocilpine Maleate / Q000378:metabolism; D004311:Double-Blind Method; D018691:Excitatory Amino Acid Antagonists / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D005260:Female; D005464:Fluorobenzenes / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D008297:Male; D010919:Placebos; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*
D018691:Excitatory Amino Acid Antagonists; D005464:Fluorobenzenes; D010919:Placebos; D016194:Receptors, N-Methyl-D-Aspartate; D016291:Dizocilpine Maleate; C405105:NPS 1506