title: NPS 1506, a moderate affinity uncompetitive NMDA receptor antagonist: preclinical summary and clinical experience.
abstract: 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).
authors.affiliation: NPS Pharmaceuticals, Inc., Salt Lake City, Utah 84108, USA.
authors.forename: A L
authors.initials: AL
authors.lastname: Mueller
authors.forename: L D
authors.initials: LD
authors.lastname: Artman
authors.forename: M F
authors.initials: MF
authors.lastname: Balandrin
authors.forename: E
authors.initials: E
authors.lastname: Brady
authors.forename: Y
authors.initials: Y
authors.lastname: Chien
authors.forename: E G
authors.initials: EG
authors.lastname: DelMar
authors.forename: A
authors.initials: A
authors.lastname: Kierstead
authors.forename: T B
authors.initials: TB
authors.lastname: Marriott
authors.forename: S T
authors.initials: ST
authors.lastname: Moe
authors.forename: J L
authors.initials: JL
authors.lastname: Raszkiewicz
authors.forename: B
authors.initials: B
authors.lastname: VanWagenen
authors.forename: D
authors.initials: D
authors.lastname: Wells
mesh_terms: 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*
chemical_list: D018691:Excitatory Amino Acid Antagonists; D005464:Fluorobenzenes; D010919:Placebos; D016194:Receptors, N-Methyl-D-Aspartate; D016291:Dizocilpine Maleate; C405105:NPS 1506