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NPS 1506, a moderate affinity uncompetitive NMDA receptor antagonist: preclinical summary and clinical experience. 2000
A L Mueller, and
L D Artman, and
M F Balandrin, and
E Brady, and
Y Chien, and
E G DelMar, and
A Kierstead, and
T B Marriott, and
S T Moe, and
J L Raszkiewicz, and
B VanWagenen, and
D Wells
NPS Pharmaceuticals, Inc., Salt Lake City, Utah 84108, USA.
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).
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