SKF-82958

SKF-82958
(IUPAC) ime
3-alil-6-hloro-1-fenil-1,2,4,5-tetrahidro-3-benzazepin-7,8-diol
Klinički podaci
Identifikatori
CAS broj 80751-65-1
ATC kod nije dodeljen
PubChem[1][2] 1225
ChemSpider[3] 1188
ChEMBL[4] CHEMBL317741
Hemijski podaci
Formula C19H20ClNO2 
Mol. masa 329,82 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

SKF-82958 je sintetičko jedinjenje iz benzazepinske klase koje deluje kao pun agonist D1/D5 receptora.[5][6] SKF-82,958 i slični selektivni puni D1 agonisti kao što su SKF-81297 i 6-Br-APB proizvode karakteristične anorektičke efekte, hiperaktivnost i samoadministraciju kod životinja, sa sličnim mada ne identičnim profilom sa dopaminergičkim stimulansima poput amfetamina.[7][8][9][10][11][12][13][14][15]

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. ↑ 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
  5. ↑ Pfeiffer, Francis R.; Wilson, James W.; Weinstock, Joseph; Kuo, George Y.; Chambers, Pamela A.; Holden, Kenneth G.; Hahn, Richard A.; Wardell, Joseph R., Jr.; Alfonso, J. Tobia; et al. (1982). „Dopaminergic activity of substituted 6-chloro-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines”. Journal of Medicinal Chemistry 25 (4): 352–358. DOI:10.1021/jm00346a005. PMID 7069713. 
  6. ↑ Wang JQ, McGinty JF (May 1997). „The full D1 dopamine receptor agonist SKF-82958 induces neuropeptide mRNA in the normosensitive striatum of rats: regulation of D1/D2 interactions by muscarinic receptors”. The Journal of Pharmacology and Experimental Therapeutics 281 (2): 972–82. PMID 9152408. 
  7. ↑ Terry P, Katz JL (1992). „Differential antagonism of the effects of dopamine D1-receptor agonists on feeding behavior in the rat”. Psychopharmacology 109 (4): 403–9. DOI:10.1007/BF02247715. PMID 1365854. 
  8. ↑ Self DW, Stein L (June 1992). „The D1 agonists SKF 82958 and SKF 77434 are self-administered by rats”. Brain Research 582 (2): 349–52. DOI:10.1016/0006-8993(92)90155-3. PMID 1356585. 
  9. ↑ Rosenzweig-Lipson S, Hesterberg P, Bergman J (September 1994). „Observational studies of dopamine D1 and D2 agonists in squirrel monkeys”. Psychopharmacology 116 (1): 9–18. DOI:10.1007/BF02244865. PMID 7862937. 
  10. ↑ Kalivas PW, Duffy P (July 1995). „D1 receptors modulate glutamate transmission in the ventral tegmental area”. Journal of Neuroscience 15 (7 Pt 2): 5379–88. PMID 7623160. 
  11. ↑ Weed MR, Woolverton WL (December 1995). „The reinforcing effects of dopamine D1 receptor agonists in rhesus monkeys”. The Journal of Pharmacology and Experimental Therapeutics 275 (3): 1367–74. PMID 8531104. 
  12. ↑ 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. 
  13. ↑ Abrahams BS, Rutherford JD, Mallet PE, Beninger RJ (February 1998). „Place conditioning with the dopamine D1-like receptor agonist SKF 82958 but not SKF 81297 or SKF 77434”. European Journal of Pharmacology 343 (2-3): 111–8. DOI:10.1016/S0014-2999(97)01531-8. PMID 9570457. 
  14. ↑ Tidey JW, Bergman J (June 1998). „Drug discrimination in methamphetamine-trained monkeys: agonist and antagonist effects of dopaminergic drugs”. The Journal of Pharmacology and Experimental Therapeutics 285 (3): 1163–74. PMID 9618419. 
  15. ↑ Berridge KC, Aldridge JW (September 2000). „Super-stereotypy I: enhancement of a complex movement sequence by systemic dopamine D1 agonists”. Synapse 37 (3): 194–204. DOI:10.1002/1098-2396(20000901)37:3<194::AID-SYN3>3.0.CO;2-A. PMID 10881041. 

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