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SKF-81297

Izvor: Wikipedija
SKF-81297
(IUPAC) ime
6-hloro-1-fenil-2,3,4,5-tetrahidro-1H-3-benzazepin-7,8-diol
Klinički podaci
Identifikatori
CAS broj 253446-15-0
ATC kod nije dodeljen
PubChem[1][2] 16219952
ChemSpider[3] 1181
Hemijski podaci
Formula C16H16ClNO2 
Mol. masa 289,76 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

SKF-81297 je sintetički lek iz benzazepinske hemijske klase, koji deluje kao selektivni agonist D1/D5 receptora. On proizvodi karakteristične stimulansne efekte: anoreksiju, hiperaktivnost i samoadministraciju kod životinja.[4] Ovakav profil ima i nekoliko srodnih lekova, kao što su 6-Br-APB i SKF-82958,[5] made ne svi D1 puni agonisti, npr. A-77636. To je posledicafunkcionalne selektivnosti D1 aktivacije.[6][7][8]

Reference

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  1. 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
  2. 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. 
  3. 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
  4. Weed MR, Vanover KE, Woolverton WL (1993). „Reinforcing effect of the D1 dopamine agonist SKF 81297 in rhesus monkeys”. Psychopharmacology 113 (1): 51–2. DOI:10.1007/BF02244333. PMID 7862828. 
  5. Weed MR, Paul IA, Dwoskin LP, Moore SE, Woolverton WL (October 1997). „The relationship between reinforcing effects and in vitro effects of D1 agonists in monkeys”. The Journal of Pharmacology and Experimental Therapeutics 283 (1): 29–38. PMID 9336305. 
  6. Chausmer AL, Katz JL (January 2002). „Comparison of interactions of D1-like agonists, SKF 81297, SKF 82958 and A-77636, with cocaine: locomotor activity and drug discrimination studies in rodents”. Psychopharmacology 159 (2): 145–53. DOI:10.1007/s002130100896. PMID 11862342. 
  7. Graham DL, Hoppenot R, Hendryx A, Self DW (April 2007). „Differential ability of D1 and D2 dopamine receptor agonists to induce and modulate expression and reinstatement of cocaine place preference in rats”. Psychopharmacology 191 (3): 719–30. DOI:10.1007/s00213-006-0473-5. PMID 16835769. 
  8. Delfino M, Kalisch R, Czisch M, Larramendy C, Ricatti J, Taravini IR, Trenkwalder C, Murer MG, Auer DP, Gershanik OS (September 2007). „Mapping the effects of three dopamine agonists with different dyskinetogenic potential and receptor selectivity using pharmacological functional magnetic resonance imaging”. Neuropsychopharmacology 32 (9): 1911–21. DOI:10.1038/sj.npp.1301329. PMID 17287822. 

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