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

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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 = 476 nM) and displaces the binding of [3H]MK-801 to rat cortical membranes (IC50 = 664 nM).

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Authors and Affiliations

  1. NPS Pharmaceuticals, Inc., Salt Lake City, Utah, U.S.A., , , , , , US

    A. L. Mueller, L. D. Artman, M. F. Balandrin, E. Brady, Y. Chien, E. G. DelMar, A. Kierstead, T. B. Marriott, S. T. Moe, J. L. Raszkiewicz, B. VanWagenen & D. Wells

Authors
  1. A. L. Mueller
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  2. L. D. Artman
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  3. M. F. Balandrin
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  4. E. Brady
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  5. Y. Chien
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  6. E. G. DelMar
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  7. A. Kierstead
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  8. T. B. Marriott
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  9. S. T. Moe
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  10. J. L. Raszkiewicz
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  11. B. VanWagenen
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  12. D. Wells
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Received August 31, 1999 Accepted September 20, 1999

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Mueller, A., Artman, L., Balandrin, M. et al. NPS 1506, a moderate affinity uncompetitive NMDA receptor antagonist: preclinical summary and clinical experience. Amino Acids 19, 177–179 (2000). https://doi.org/10.1007/s007260070047

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  • DOI: https://doi.org/10.1007/s007260070047

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