SKF-83,959 je sintetički benzazepinski derivat koji se koristi u naučnim istraživanjima. On deluje kao selektivni antagonist D1 receptor i pun agonist D5 receptora. On ima visok afinitet za oba receptora, te stimuliše putem D5 receptora PLC/PI put sekundarnog glasnika bez uticaja na cAMP/AC put, koji je povezan sa D1 receptorom.[5][6][7][8]
SKF-83959
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(IUPAC) ime
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6-hloro-7,8-dihidroksi-3-metil-1-(3-metilfenil)-2,3,4,5-tetrahidro-1H-3-benzazepin
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Klinički podaci
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Identifikatori
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ATC kod
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nije dodeljen
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PubChem[1][2]
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24278699
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ChemSpider[3]
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10131933
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ChEMBL[4]
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CHEMBL520992 Y
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Hemijski podaci
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Formula
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C18H20ClNO2
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Mol. masa
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317,810 g/mol
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SMILES
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eMolekuli & PubHem
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InChI |
InChI=1S/C18H20ClNO2.BrH/c1-11-4-3-5-12(8-11)15-10-20(2)7-6-13-14(15)9-16(21)18(22)17(13)19;/h3-5,8-9,15,21-22H,6-7,10H2,1-2H3;1H Y Key: FHYWNBUFNGHNCP-UHFFFAOYSA-N Y |
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Farmakoinformacioni podaci
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Trudnoća
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?
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Pravni status
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- ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
- ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
- ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
- ↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
- ↑ Jin LQ, Goswami S, Cai G, Zhen X, Friedman E (April 2003). „SKF83959 selectively regulates phosphatidylinositol-linked D1 dopamine receptors in rat brain”. Journal of Neurochemistry 85 (2): 378–86. PMID 12675914.
- ↑ Zhen X, Goswami S, Friedman E (April 2005). „The role of the phosphatidyinositol-linked D1 dopamine receptor in the pharmacology of SKF83959”. Pharmacology, Biochemistry, and Behavior 80 (4): 597–601. DOI:10.1016/j.pbb.2005.01.016. PMID 15820529.
- ↑ Zhang ZJ, Jiang XL, Zhang SE, Hough CJ, Li H, Chen JG, Zhen XC (2005). „The paradoxical effects of SKF83959, a novel dopamine D1-like receptor agonist, in the rat acoustic startle reflex paradigm”. Neuroscience Letters 382 (1-2): 134–8. DOI:10.1016/j.neulet.2005.03.001. PMID 15911136.
- ↑ Sahu A, Tyeryar KR, Vongtau HO, Sibley DR, Undieh AS (March 2009). „D5 dopamine receptors are required for dopaminergic activation of phospholipase C”. Molecular Pharmacology 75 (3): 447–53. DOI:10.1124/mol.108.053017. PMID 19047479. [mrtav link]