A novel N-methyl-D-aspartate receptor open channel blocker with in vivo neuroprotectant activity

Journal of Pharmacology and Experimental Therapeutics

Volumn 302, Issue 1, 2002, Pages 163-173

  Planells Cases, Rosa ^a   Montoliu, Carmina ^b   Humet, Marc ^c   Fernández, Asia M ^a   García Martínez, Carolina ^a   Valera, Elvira ^d   Merino, Jaime M ^d   Pérez Payá, Enrique ^e   Messeguer, Angel ^c   Felipo, Vicente ^b   Ferrer Montiel, Antonio ^a  

^a MIGUEL HERNÁNDEZ UNIVERSITY   (Spain)

^b Laboratorio de Neurobiologia de Prince Felipe Research Centre   (Spain)

^c DEPARTMENT OF ENVIRONMENTAL CHEMISTRY   (Spain)

^d UNIVERSITY OF EXTREMADURA   (Spain)

^e UNIVERSITY OF VALENCIA   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

3,3 DIPHENYLPROPYL N GLYCINAMIDE; CYCLIC GMP; DIZOCILPINE; GLUTAMIC ACID; GLYCINE DERIVATIVE; N METHYL DEXTRO ASPARTIC ACID RECEPTOR; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT; NITRIC OXIDE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING KINETICS; CELL PROTECTION; CEREBELLUM; CHANNEL GATING; CONTROLLED STUDY; DRUG EFFICACY; EMBRYO; HIPPOCAMPUS; MALE; MOUSE; NERVE CELL NECROSIS; NEUROPROTECTION; NEUROTOXICITY; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY;

AMMONIA; ANIMALS; CELL DEATH; CELLS, CULTURED; CEREBELLUM; CYCLIC AMP; CYCLIC GMP; DOSE-RESPONSE RELATIONSHIP, DRUG; DOWN-REGULATION; EXCITATORY AMINO ACID ANTAGONISTS; GLYCINE; HIPPOCAMPUS; NEURONS; NEUROPROTECTIVE AGENTS; NITRIC OXIDE; OOCYTES; RATS; RECEPTORS, N-METHYL-D-ASPARTATE; RECOMBINANT PROTEINS; XENOPUS;

EID: 0036089218     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.302.1.163     Document Type: Article

References (41)

1. Trapping channel block of NMDA-activated responses by amantadine and memantine
2. Ligands for glutamate receptors: Design and therapeutic prospects
3. Antiparkinsonian and antidyskinetic activity of drugs targeting central glutamatergic mechanisms
4. Neuroprotective concentrations of the N-methyl-D-aspartate open-channel blocker memantine are effective without cytoplasmic vacuolation following post-ischemic administration and do not block maze learning or longterm potentiation
5. Antagonists selective for NMDA receptors containing the NR2B subunit
6. The role of glutamate excitotoxicity in hypoxicischemic neuronal death
7. An oral vaccine against NMDAR1 with efficacy in experimental stroke and epilepsy
8. Selected peptides targeted to the NMDA receptor channel protect neurones from excitotoxic death
9. Structural determinants of the blocker binding site in glutamate and NMDA receptor channel
10. Engineering the NMDA receptor channel lining
11. Ro25-6981, a highly potent and selective blocker of N-methyl-Daspartate receptors containing NR2B subunit. Characterization in vitro
12. Attenuation of thermal nociception and hyperalgesia by VR1 blockers
13. Insights from mouse models into the molecular basis of neurodegeneration
14. A combinatorial peptoid library for the identification of novel MSH and GRP/bombesin receptor ligands
15. NMDA receptor antagonists prevent acute ammonia toxicity in mice
16. Chronic hyperammonemia impairs the glutamate-nitric oxidecyclic GMP pathway in cerebellar neurones in culture and in rat in vivo
17. Block of N-methyl-D-aspartate activated current by the anticonvulsant MK-801: Selective binding to open channels
18. Neuronal death enhanced by N-methyl-D-aspartate antagonists
19. The mitochondrial death/life regulator in apoptosis and necrosis
20. Potential and current use of N-methyl-D-aspartate (NMDA) receptor antagonists in diseases of aging
21. The changing landscape of ischaemic brain injury mechanisms
22. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
23. Excitatory amino acids as a final common pathway for neurologic disorders
24. Ammonia prevents activation of NMDA receptors in rat cerebellar neuronal cultures
25. Nicotine prevents glutamate-induced proteolysis of the microtubule-associated protein MAP-2 and glutamate neurotoxicity in primary cultures of cerebellar neurones
26. Role of cyclic GMP in glutamate neurotoxicity in primary cultures of cerebellar neurones
27. Molecular diversity in drug design
28. Neuronal necrosis and apoptosis: Two distinct events induced by exposure to glutamate or oxidative stress
29. Peptomers: A versatile approach for the preparation of diverse combinatorial peptidomimetic bead libraries
30. Blood-brain barrier biology and methodology
31. Amino-alkyl-cyclohexanes are novel uncompetitive NMDA receptor antagonists with strong voltage-dependency and fast blocking kinetics: In vitro and in vivo characterization
32. Memantine is a clinically well tolerated N-methyl-D-aspartate (NMDA) receptor antagonist-a review of preclinical data
33. Identification of a high affinity divalent cation binding site near the entrance of the NMDA receptor
34. Glutamate antagonists limit tumor growth
35. Mitochondrial dysfunction is a primary event in glutamate neurotoxicity
36. An N-methyl-D-aspartate receptor channel blocker with neuroprotective activity
37. Glutamate release promotes growth of malignant gliomas
38. Ionic blockage of sodium channels in nerve
39. Structural basis for explaining open-channel blockade of the NMDA receptor