Matches in DBpedia 2016-04 for { <http://dbpedia.org/resource/Rapastinel> ?p ?o }
- Rapastinel abstract "Rapastinel (INN) (code name GLYX-13) is an intravenously-administered, selective, weak partial agonist of the glycine site of the NMDA receptor (IA ≈ 25%) which is under development by Naurex as an adjunctive therapy for treatment-resistant depression. It is an amidated tetrapeptide (Thr-Pro-Pro-Thr-NH2) which rapidly crosses the blood-brain-barrier, but is not active orally. On March 3, 2014 the U.S. FDA granted Fast Track designation to the development of rapastinel as an adjunctive therapy in treatment-resistant major depressive disorder. As of 2015, the drug has completed phase II clinical development for this indication. Phase III clinical trials were expected to be starting in 2015. By Jan. 29, 2016 Allergan plc. (who acquired Naurex in July 2015) announced that its meanwhile Phase III ready investigational medication rapastinel (GLYX-13) received Breakthrough Therapy designation from the U.S. FDA for adjunctive treatment of major depressive disorder.In addition to its antidepressant effects, rapastinel has been shown to enhance memory and learning in both young adult and learning-impaired, aging rat models. It has been shown to increase Schaffer collateral-CA1 long-term potentiation in vitro. In concert with a learning task, rapastinel has also been shown to elevate gene expression of hippocampal NR1, a subunit of the NMDA receptor, in 3-month-old rats. Neuroprotective effects have also been demonstrated in Mongolian Gerbils by delaying the death of CA1, CA3, and dentate gyrus pyramidal neurons under glucose and oxygen-deprived conditions. Additionally, rapastinel has demonstrated antinociceptive activity, which is of particular interest, as both competitive and noncompetitive NMDA receptor antagonists are ataxic at analgesic doses, while rapastinel and other glycine subunit ligands are able to elicit analgesia at sub-ataxic doses.Rapastinel does not actually bind to the glycine site of the NMDA receptor, but rather to a site on the NMDA receptor that allosterically modulates the glycine site. As such, rapastinel is technically a partial negative allosteric modulator of the glycine site of the NMDA receptor, or a functional glycine site partial agonist.".
- Rapastinel atcPrefix "none".
- Rapastinel casNumber "117928-94-6".
- Rapastinel iupacName "(S)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-1-[(S)-1-((2S,3R)-2-amino-3-hydroxybutanoyl)pyrrolidine-2-carbonyl]pyrrolidine-2-carboxamide".
- Rapastinel pubchem "14539800".
- Rapastinel thumbnail Rapastinel.svg?width=300.
- Rapastinel wikiPageExternalLink allergan-s-rapastinel-receives-fda-breakthrough-th.
- Rapastinel wikiPageExternalLink glyx-13.
- Rapastinel wikiPageID "37227776".
- Rapastinel wikiPageLength "8195".
- Rapastinel wikiPageOutDegree "46".
- Rapastinel wikiPageRevisionID "707012220".
- Rapastinel wikiPageWikiLink 4-Chlorokynurenine.
- Rapastinel wikiPageWikiLink Allosteric_modulator.
- Rapastinel wikiPageWikiLink Analgesic.
- Rapastinel wikiPageWikiLink Ataxia.
- Rapastinel wikiPageWikiLink Binding_selectivity.
- Rapastinel wikiPageWikiLink Blood–brain_barrier.
- Rapastinel wikiPageWikiLink Breakthrough_therapy.
- Rapastinel wikiPageWikiLink samidorphan.
- Rapastinel wikiPageWikiLink CERC-301.
- Rapastinel wikiPageWikiLink Category:Antidepressants.
- Rapastinel wikiPageWikiLink Category:NMDA_receptor_agonists.
- Rapastinel wikiPageWikiLink Category:Nootropics.
- Rapastinel wikiPageWikiLink Category:Peptides.
- Rapastinel wikiPageWikiLink Clinical_trial.
- Rapastinel wikiPageWikiLink Combination_therapy.
- Rapastinel wikiPageWikiLink Dentate_gyrus.
- Rapastinel wikiPageWikiLink Esketamine.
- Rapastinel wikiPageWikiLink FDA_Fast_Track_Development_Program.
- Rapastinel wikiPageWikiLink GRIN1.
- Rapastinel wikiPageWikiLink Glycine.
- Rapastinel wikiPageWikiLink Hippocampus_anatomy.
- Rapastinel wikiPageWikiLink In_vitro.
- Rapastinel wikiPageWikiLink International_nonproprietary_name.
- Rapastinel wikiPageWikiLink Intravenous_therapy.
- Rapastinel wikiPageWikiLink Intrinsic_activity.
- Rapastinel wikiPageWikiLink Ligand_(biochemistry).
- Rapastinel wikiPageWikiLink Long-term_potentiation.
- Rapastinel wikiPageWikiLink Major_depressive_disorder.
- Rapastinel wikiPageWikiLink Mongolian_gerbil.
- Rapastinel wikiPageWikiLink NMDA_receptor.
- Rapastinel wikiPageWikiLink NRX-1074.
- Rapastinel wikiPageWikiLink NSI-189.
- Rapastinel wikiPageWikiLink Naurex.
- Rapastinel wikiPageWikiLink Neboglamine.
- Rapastinel wikiPageWikiLink Oral_administration.
- Rapastinel wikiPageWikiLink Partial_agonist.
- Rapastinel wikiPageWikiLink Pharmaceutical_drug.
- Rapastinel wikiPageWikiLink Phases_of_clinical_research.
- Rapastinel wikiPageWikiLink Pyramidal_cell.
- Rapastinel wikiPageWikiLink Schaffer_collateral.
- Rapastinel wikiPageWikiLink Tetrapeptide.
- Rapastinel wikiPageWikiLink Treatment-resistant_depression.
- Rapastinel wikiPageWikiLinkText "Rapastinel".
- Rapastinel wikiPageWikiLinkText "rapastinel".
- Rapastinel atcPrefix "none".
- Rapastinel c "18".
- Rapastinel casNumber "117928".
- Rapastinel chemspiderid "25069944".
- Rapastinel h "31".
- Rapastinel image "GLYX-133Dan.gif".
- Rapastinel inchi "1".
- Rapastinel inchikey "GIBQQARAXHVEGD-BSOLPCOYBZ".
- Rapastinel iupacName "-N-[-1-amino-3-hydroxy-1-oxobutan-2-yl]-1-[-1-pyrrolidine-2-carbonyl]pyrrolidine-2-carboxamide".
- Rapastinel legalStatus "Investigational New Drug".
- Rapastinel molecularWeight "413.47".
- Rapastinel n "5".
- Rapastinel o "6".
- Rapastinel pregnancyUs "N".
- Rapastinel pubchem "14539800".
- Rapastinel smiles "C[C@H]O".
- Rapastinel stdinchi "1".
- Rapastinel stdinchikey "GIBQQARAXHVEGD-BSOLPCOYSA-N".
- Rapastinel width "200".
- Rapastinel width "250".
- Rapastinel wikiPageUsesTemplate Template:Antidepressants.
- Rapastinel wikiPageUsesTemplate Template:Drugbox.
- Rapastinel wikiPageUsesTemplate Template:Glutamatergics.
- Rapastinel wikiPageUsesTemplate Template:Nervous-system-drug-stub.
- Rapastinel wikiPageUsesTemplate Template:Nootropics.
- Rapastinel wikiPageUsesTemplate Template:Reflist.
- Rapastinel subject Category:Antidepressants.
- Rapastinel subject Category:NMDA_receptor_agonists.
- Rapastinel subject Category:Nootropics.
- Rapastinel subject Category:Peptides.
- Rapastinel hypernym Agonist.
- Rapastinel type ChemicalSubstance.
- Rapastinel type Drug.
- Rapastinel type Agonist.
- Rapastinel type Chemical.
- Rapastinel type Drug.
- Rapastinel type ChemicalObject.
- Rapastinel type Thing.
- Rapastinel type Q8386.
- Rapastinel comment "Rapastinel (INN) (code name GLYX-13) is an intravenously-administered, selective, weak partial agonist of the glycine site of the NMDA receptor (IA ≈ 25%) which is under development by Naurex as an adjunctive therapy for treatment-resistant depression. It is an amidated tetrapeptide (Thr-Pro-Pro-Thr-NH2) which rapidly crosses the blood-brain-barrier, but is not active orally. On March 3, 2014 the U.S.".
- Rapastinel label "Rapastinel".
- Rapastinel sameAs Q5513673.
- Rapastinel sameAs m.0n52q16.
- Rapastinel sameAs Q5513673.