RPR 119990, a novel α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid antagonist: Synthesis, pharmacological properties, and activity in an animal model of amyotrophic lateral sclerosis

Journal of Pharmacology and Experimental Therapeutics

Volumn 299, Issue 1, 2001, Pages 314-322

  Canton, Thierry ^a   Böhme, Georg Andrees ^a   Boireau, Alain ^a   Bordier, Françoise ^a   Mignani, Serge ^a   Jimonet, Patrick ^a   Jahn, Ghafoor ^a   Alavijeh, Mohammad ^a   Stygall, James ^a   Roberts, Simon ^a   Brealey, Clive ^a   Vuilhorgne, Marc ^a   Debono, Marc William ^a   Le Guern, Sylvain ^a   Laville, Michel ^a   Briet, Dominique ^a   Roux, Michel ^a   Stutzmann, Jean Marie ^a   Pratt, Jeremy ^a  

^a SANOFI   (France)

Author keywords

[No Author keywords available]

Indexed keywords

9 CARBOXYMETHYL 4 OXO 5H,10H IMIDAZO[1,2 E]INDENO[1,2 E]PYRAZIN 2 PHOSPHONIC ACID; AMPA RECEPTOR ANTAGONIST; ANTICONVULSIVE AGENT; PHOSPHONIC ACID DERIVATIVE; RPR 119990; UNCLASSIFIED DRUG;

AMINO ACID TRANSPORT; AMYOTROPHIC LATERAL SCLEROSIS; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTICONVULSANT ACTIVITY; ARTICLE; BRAIN CORTEX; DISEASE MODEL; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG EFFECT; DRUG ELIMINATION; DRUG MECHANISM; DRUG SYNTHESIS; ELECTRIC SHOCK; EVOKED CORTICAL RESPONSE; GRIP STRENGTH; HIPPOCAMPUS; ION CURRENT; MALE; MUSCLE STRENGTH; NONHUMAN; OOCYTE; PRIORITY JOURNAL; RAT; TRANSGENIC MOUSE; XENOPUS LAEVIS;

AMYOTROPHIC LATERAL SCLEROSIS; ANIMALS; ANTICONVULSANTS; DISEASE PROGRESSION; ELECTROPHYSIOLOGY; ELECTROSHOCK; EXCITATORY AMINO ACID ANTAGONISTS; GLUTAMIC ACID; IMIDAZOLES; LONGEVITY; MICE; MICE, TRANSGENIC; MUSCLE, SKELETAL; NEURONS; PATCH-CLAMP TECHNIQUES; PYRAZINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, AMPA; SUPEROXIDE DISMUTASE;

EID: 0034802145     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (32)

1. The role of calcium-binding proteins in selective motoneuron vulnerability in amyotrophic lateral sclerosis
2. Immunoglobulins from motoneurone disease patients enhance glutamate release from rat hippocampal neurones in culture
3. A controlled trial of riluzole in amyotrophic lateral sclerosis
4. Neuropharmacology of AMPA and kainate receptors
5. Neuroprotective effects of RPR 104632, a novel antagonist at the glycine site of the NMDA receptor, in vitro
6. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding
7. Glutamate uptake is decreased tardively in the spinal cord of familial ALS mice
8. Calcium-mediated neurotoxicity: Relationship to specific channel types and role in ischemic damage
9. Glutamate neurotoxicity and diseases of the nervous system
10. Cell culture evidence for the neuronal degeneration in amyotrophic lateral sclerosis being linked to glutamate AMPA/kainate receptors
11. Synthesis of [3]2-amino-4-phosphanobutyric acid and characterization of its binding to rat brain membranes: A selective ligand for the chloride/calcium-dependent class of L-glutamate binding sites
12. Inhibition by riluzole of electrophysiological responses mediated by rat kainate and NMDA receptors expressed in Xenopus oocytes
13. Effects of riluzole on glutamatergic neurotransmission in the mammalian central nervous system, and other pharmacological effects
14. 3-Amino- and 3-cyano-1,2,4-oxadiazole
15. Benefit of vitamin E, riluzole and gabapentin in a transgenic model of amyotrophic lateral sclerosis
16. Riluzole preserves motor function in a transgenic model of familial amyotrophic lateral sclerosis
17. Motor neuron degeneration in mice expressing a human Cu, Zn superoxide dismutase mutation
18. Chaotropic ions affect the conformation of quisqualate receptors in rat cortical membranes
19. Neuromuscular function impairment is not caused by motor neurone loss in familial ALS mice: An electromyographic study
20. The degenerated side chain approach to the carbon analogue of the Claisen rearrangement. Formation of nine-membered rings by the sterically accelerated ene reaction
21. Excitatory amino acid receptors, second messengers and regulation of intracellular calcium in mammalian neurons
22. The NBQX story
23. Decreased glutamate transport by the brain and spinal cord in amyotrophic lateral sclerosis
24. Excitotoxicity and motor neurone disease: A review of the evidence
25. Guam amyotrophic lateral sclerosis-parkinsonism-dementia linked to a plant excitant neurotoxin
26. Lathyrism: Evidence for role of the neuroexcitatory aminoacid BOAA
27. Neuroprotective efficacy of YM872, an alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptor antagonist, after permanent middle cerebral artery occlusion in rats
28. ZK 200775: A phosphanate quinoxalinedione AMPA antagonist for neuroprotection in stroke and trauma
29. 2+ permeable AMPA or kainate receptors: Possible key factors in selective neurodegeneration
30. Calcium permeable an alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors: A molecular determinant of selective vulnerability in amyotrophic lateral sclerosis