Извор странице Likostinel

{{Drugbox
| IUPAC_name        = 6,7-Dihloro-5-nitro-1,4-dihidro-2,3-hinoksalindion
| 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
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 3Z3037LJTC
| ATC_prefix        = None
| ATC_suffix        = 
| PubChem           = 5486198
| DrugBank          = 
| ChemSpiderID      = 4588899
| chemical_formula =
| C=8 | H=3 | Cl=2 | N=3 | O=4 
| 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      =  <!-- A / B1 / B2 / B3 / C / D / X -->
| pregnancy_US      =  <!-- A / B            / C / D / X -->
| pregnancy_category=  
| legal_AU =  <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled-->
| legal_CA =  <!-- Schedule I, II, III, IV, V, VI, VII, VIII -->
| legal_UK =  <!-- GSL, P, POM, CD, or Class A, B, C -->
| legal_US =  <!-- OTC / Rx-only / Schedule I, II, III, IV, V -->
| legal_status      = 
| routes_of_administration = 
}}

'''Licostinel''' ([[Међународни незаштићени назив|INN]]) (kodni naziv '''ACEA-1021''') je [[antagonist (farmakologija)|kompetitivni]], [[antagonist (farmakologija)|tihi antagonist]] [[nMDA receptor|glicinskog mesta]] [[NMDA receptor|NMDA receptora]] (K<sub>b</sub> = 5 nM).<ref name="GillPulido2007">{{cite book| vauthors = Small DL, Tauskela JS | chapter = Glutamate Receptor Pharmacology: Lessons Learned from the Last Decade of Stroke Trials | veditors = Gill S, Pulido O |title=Glutamate Receptors in Peripheral Tissue: Excitatory Transmission Outside the CNS|chapter-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–}}</ref><ref name="GusevSkvortsova2003">{{cite book| vauthors = Gusev EI, Skvortsova VI | chapter = Primary Neuroprotection |title=Brain Ischemia| chapter-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–}}</ref><ref name="pmid8643094">{{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 = Molecular Pharmacology | volume = 49 | issue = 3 | pages = 540–546 | date = March 1996 | pmid = 8643094 | url = http://molpharm.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8643094 }}</ref> Bio je pod istragom od strane Acea Pharmaceuticals kao [[neuroprotective agent|neuroprotektivni agens]] za lečenje [[akutna ishemija mozga|cerebralne ishemije]] povezane sa [[мождани удар|moždanim udarom]] i [[head injury|povredama glave]], ali nikada nije plasiran na tržište.<ref name="GillPulido2007" /><ref name="GusevSkvortsova2003" /><ref name="SirinathsinghjiHill2002">{{cite book| vauthors = Boyce SG, Rupniak N | chapter = Behavioural studies on the potential of NMDA receptor antagonists as analgesics | veditors = Sirinathsinghji DJ, Hill RG |title=NMDA Antagonists As Potential Analgesic Drugs|chapter-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–}}</ref> U [[kliničko ispitivanje|kliničkim ispitivanjima]], likostinel nije proizveo [[психотомиметизам|psihotomimetičke]] efekte slične [[фенциклидин|fenciklidinu]] u testiranim dozama, iako je primećena prolazna [[седација|sedacija]], [[вртоглавица|vrtoglavica]] i [[мучнина|mučnina]].<ref name="SirinathsinghjiHill2002"/><ref name="BountraMunglani2013">{{cite book| vauthors = Chizh BA, Headly PM | chapter = N-Methyl-D-Aspartate (NMDA) Receptors as Target for Pain Therapy | veditors = Bountra C, Munglani R, Schmidt WK |title=Pain: Current Understanding, Emerging Therapies, and Novel Approaches to Drug Discovery| chapter-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–}}</ref> Pored svog delovanja na NMDA receptor, likostinel takođe deluje kao antagonist [[AMPA receptor|AMPA]] i [[kainatni receptor|kainatnog receptora]] u visokim koncentracijama (K<sub>b</sub> = 0.9 μM i 2,5 μM, respektivno).<ref name="pmid8643094" />

== Reference ==
{{Reflist}}

{{Glutamatergični ligandi-lat}}
{{Modulatori jonotropnog glutamatnog receptora-lat}}
{{Authority control-lat}}
{{portal bar-lat|Hemija}}

[[Категорија:Неуропротективни агенси]]
[[Категорија:Антагонисти NMDA рецептора]]
[[Категорија:Антагонисти каинатних рецептора]]
[[Категорија:Лекови без АТЦ кода]]
[[Категорија:Нитро једињења]]
[[Категорија:Хлороарени]]
[[Категорија:Хиноксалини]]