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)...

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Bibliographic Details
Published in:Amino acids 2000-01, Vol.19 (1), p.177-179
Main Authors: Mueller, A L, Artman, L D, Balandrin, M F, Brady, E, Chien, Y, DelMar, E G, Kierstead, A, Marriott, T B, Moe, S T, Raszkiewicz, J L, VanWagenen, B, Wells, D
Format: Article
Language:English
Subjects:
Adolescent
Adult
Affinity
Animals
Antagonist drugs
Calcium
Cells, Cultured
Cerebellum
Cerebral Cortex - cytology
Cerebral Cortex - drug effects
Cerebral Cortex - metabolism
Dizocilpine
Dizocilpine Maleate - metabolism
Double-Blind Method
Excitatory Amino Acid Antagonists - adverse effects
Excitatory Amino Acid Antagonists - pharmacokinetics
Excitatory Amino Acid Antagonists - pharmacology
Excitatory Amino Acid Antagonists - therapeutic use
Female
Fluorobenzenes - adverse effects
Fluorobenzenes - pharmacokinetics
Fluorobenzenes - pharmacology
Fluorobenzenes - therapeutic use
Glutamic acid receptors (ionotropic)
Glycine
Granule cells
Humans
Male
N-Methyl-D-aspartic acid receptors
Placebos
Rats
Receptors
Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors
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Description
Summary: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).
ISSN:0939-4451
1438-2199
DOI:10.1007/s007260070047