| 词条 | Licostinel |
| 释义 |
| IUPAC_name = 6,7-Dichloro-5-nitro-1,4-dihydro-2,3-quinoxalinedione | image = Licostinel.svg | alt = Skeletal formula | width = 180 | image2 = Licostinel molecule spacefill.png | alt2 = Ball-and-stick model of licostinel | CAS_number = 153504-81-5 | ATC_prefix = None | ATC_suffix = | PubChem = 5486198 | DrugBank = | ChemSpiderID = 4588899 | chemical_formula = | C=8 | H=3 | Cl=2 | N=3 | O=4 | molecular_weight = 276.033 g/mol | SMILES = c1c2c(c(c(c1Cl)Cl)[N+](=O)[O-])[nH]c(=O)c(=O)[nH]2 | StdInChI = 1S/C8H3Cl2N3O4/c9-2-1-3-5(6(4(2)10)13(16)17)12-8(15)7(14)11-3/h1H,(H,11,14)(H,12,15) | StdInChIKey = CHFSOFHQIZKQCR-UHFFFAOYSA-N | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | pregnancy_AU = | pregnancy_US = | pregnancy_category= | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = }}Licostinel (INN) (code name ACEA-1021) is a competitive, silent antagonist of the glycine site of the NMDA receptor (Kb = 5 nM).[1][2][3][3] It was under investigation by Acea Pharmaceuticals as a neuroprotective agent for the treatment of cerebral ischemia associated with stroke and head injuries but was ultimately never marketed.[1][2][4] In clinical trials, licostinel did not produce phencyclidine-like psychotomimetic effects at the doses tested, though transient sedation, dizziness, and nausea were observed.[4][5] In addition to its actions at the NMDA receptor, licostinel also acts as an antagonist of the AMPA and kainate receptors at high concentrations (Kb = 0.9 µM and 2.5 µM, respectively).[3] See also
References1. ^1 {{cite book|author1=Santokh Gill|author2=Olga Pulido|title=Glutamate Receptors in Peripheral Tissue: Excitatory Transmission Outside the CNS|url=https://books.google.com/books?id=wcjiZ58mypIC&pg=PA36|date=31 January 2007|publisher=Springer Science & Business Media|isbn=978-0-306-48644-9|pages=36–}} {{Ionotropic glutamate receptor modulators}}{{nervous-system-drug-stub}}2. ^1 {{cite book|author1=Eugene I. Gusev|author2=Veronika I. Skvortsova|title=Brain Ischemia|url=https://books.google.com/books?id=TLla0xisFkoC&pg=PA249|date=30 April 2003|publisher=Springer Science & Business Media|isbn=978-0-306-47694-5|pages=249–}} 3. ^1 2 {{cite journal | vauthors = Wilding TJ, Huettner JE | title = Antagonist pharmacology of kainate- and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-preferring receptors | journal = Mol. Pharmacol. | volume = 49 | issue = 3 | pages = 540–6 | year = 1996 | pmid = 8643094 | doi = | url = http://molpharm.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8643094}} 4. ^1 {{cite book|author1=Dalip J. S. Sirinathsinghji|author2=Ray G. Hill|title=Nmda Antagonists As Potential Analgesic Drugs|url=https://books.google.com/books?id=pIDGlb1ISCgC&pg=PA151|date=1 January 2002|publisher=Springer Science & Business Media|isbn=978-3-7643-6011-5|pages=151–}} 5. ^{{cite book|author1=Chas Bountra|author2=Rajesh Munglani|author3=William K. Schmidt|title=Pain: Current Understanding, Emerging Therapies, and Novel Approaches to Drug Discovery|url=https://books.google.com/books?id=anRzslvfcUwC&pg=PA567|date=28 May 2013|publisher=CRC Press|isbn=978-0-203-91125-9|pages=567–}} 8 : AMPA receptor antagonists|Kainate receptor antagonists|Ketones|Nitro compounds|Neuroprotective agents|NMDA receptor antagonists|Chloroarenes|Quinoxalines |
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