NPS 1506, a moderate affinity uncompetitive NMDA receptor antagonist: preclinical summary and clinical experience
| Autor: | Y. Chien, M. F. Balandrin, S. T. Moe, D. Wells, T. B. Marriott, A. Kierstead, E. Brady, B. VanWagenen, E. G. Delmar, J. L. Raszkiewicz, Alan L. Mueller, Linda D. Artman |
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| Rok vydání: | 2000 |
| Předmět: |
Adult
Male Adolescent Clinical Biochemistry Pharmacology Biochemistry Neuroprotection Receptors N-Methyl-D-Aspartate Placebos Double-Blind Method Animals Humans IC50 Cells Cultured Cerebral Cortex Chemistry Organic Chemistry technology industry and agriculture Antagonist Glutamate receptor Rats Fluorobenzenes Membrane NMDA receptor Female Dizocilpine Maleate Excitatory Amino Acid Antagonists Cytosolic calcium |
| Zdroj: | Amino acids. 19(1) |
| ISSN: | 0939-4451 |
| Popis: | 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). |
| Databáze: | OpenAIRE |
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