NPS 1506, a moderate affinity uncompetitive NMDA receptor antagonist: preclinical summary and clinical experience

Authors
Mueller, AL Artman, LD Balandrin, MF Brady, E Chien, Y DelMar, EG Kierstead, A Marriott, TB Moe, ST Raszkiewicz, JL VanWagenen, B Wells, D
Citation
Al. Mueller et al., NPS 1506, a moderate affinity uncompetitive NMDA receptor antagonist: preclinical summary and clinical experience, AMINO ACIDS, 19(1), 2000, pp. 177-179
Categorie Soggetti
Biochemistry & Biophysics
Journal title
AMINO ACIDS
ISSN journal
09394451 → ACNP
Volume
19
Issue
1
Year of publication
2000
Pages
177 - 179
Database
ISI
SICI code
0939-4451(2000)19:1<177:N1AMAU>2.0.ZU;2-Q
Abstract
NPS Pharmaceuticals, Inc. (NPS) has synthesized a series of openchannel blo ckers with varying potencies at the NMDA receptor. NPS 1506 (Fig. 1) is a m oderate affinity antagonist that inhibits NMDA/glycine-induced increases in cytosolic calcium in cultured rat cerebellar granule cells (IC50 = 476nM) and displaces the binding of [H-3]MK-801 to rat cortical membranes (IC50 = 664nM).