Likostinel
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| IUPAC ime | |
|---|---|
6,7-Dihloro-5-nitro-1,4-dihidro-2,3-hinoksalindion | |
| Identifikatori | |
| CAS broj | 153504-81-5 |
| ATC kod | None |
| PubChem | CID 5486198 |
| ChemSpider | 4588899 |
| UNII | 3Z3037LJTC  |
| Hemijski podaci | |
| Formula | C8H3Cl2N3O4 |
| Molarna masa | 276,03 g·mol−1 |
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Licostinel (INN) (kodni naziv ACEA-1021) je kompetitivni, tihi antagonist glicinskog mesta NMDA receptora (Kb = 5 nM).[1][2][3] Bio je pod istragom od strane Acea Pharmaceuticals kao neuroprotektivni agens za lečenje cerebralne ishemije povezane sa moždanim udarom i povredama glave, ali nikada nije plasiran na tržište.[1][2][4] U kliničkim ispitivanjima, likostinel nije proizveo psihotomimetičke efekte slične fenciklidinu u testiranim dozama, iako je primećena prolazna sedacija, vrtoglavica i mučnina.[4][5] Pored svog delovanja na NMDA receptor, likostinel takođe deluje kao antagonist AMPA i kainatnog receptora u visokim koncentracijama (Kb = 0.9 μM i 2,5 μM, respektivno).[3]
Reference
[uredi | uredi izvor]- ^ a b Small DL, Tauskela JS (31. 1. 2007). „Glutamate Receptor Pharmacology: Lessons Learned from the Last Decade of Stroke Trials”. Ur.: Gill S, Pulido O. Glutamate Receptors in Peripheral Tissue: Excitatory Transmission Outside the CNS. Springer Science & Business Media. str. 36—. ISBN 978-0-306-48644-9.
- ^ a b Gusev EI, Skvortsova VI (30. 4. 2003). „Primary Neuroprotection”. Brain Ischemia. Springer Science & Business Media. str. 249—. ISBN 978-0-306-47694-5.
- ^ a b Wilding TJ, Huettner JE (mart 1996). „Antagonist pharmacology of kainate- and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-preferring receptors”. Molecular Pharmacology. 49 (3): 540—546. PMID 8643094.
- ^ a b Boyce SG, Rupniak N (1. 1. 2002). „Behavioural studies on the potential of NMDA receptor antagonists as analgesics”. Ur.: Sirinathsinghji DJ, Hill RG. NMDA Antagonists As Potential Analgesic Drugs. Springer Science & Business Media. str. 151—. ISBN 978-3-7643-6011-5.
- ^ Chizh BA, Headly PM (28. 5. 2013). „N-Methyl-D-Aspartate (NMDA) Receptors as Target for Pain Therapy”. Ur.: Bountra C, Munglani R, Schmidt WK. Pain: Current Understanding, Emerging Therapies, and Novel Approaches to Drug Discovery. CRC Press. str. 567—. ISBN 978-0-203-91125-9.
