SB-277011-A

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(Preusmjereno sa SB-277,011-A)
SB-277011-A
(IUPAC) ime
N'trans-4-[2-(6-cijano-3,4-dihidroizohinolin-2(1H)-il)etil]cikloheksil}hinolin-4-karboksamid
Klinički podaci
Identifikatori
ATC kod  ?
PubChem[1][2] 5311096
ChEMBL[3] CHEMBL85606 YesY
Hemijski podaci
Formula C28H30N4O 
Mol. masa 438,563 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

SB-277,011A je lek koji deluje kao potentan i selektivan antagonist dopaminkog D3 receptor receptora.[4] On je oko 80-100 puta selektivniji za D3 u odnosu na D2.[5] On nije parcijalni agonist.[6]

SB-277,011A se koristi za studiranje adikcije na stimulišuće droge poput nikotina[7] i kokaina.[8][9]

Reference[uredi - уреди | uredi izvor]

  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. 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. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  4. Stemp G, Ashmeade T, Branch CL, Hadley MS, Hunter AJ, Johnson CN, Nash DJ, Thewlis KM, Vong AK (2000). "Design and synthesis of trans-N-4-2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethylcyclohexyl-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat". Journal of medicinal chemistry 43 (9): 1878–85. PMID 10794704. doi:10.1021/jm000090i. 
  5. Southam E, Lloyd A, Jennings CA, Cluderay JE, Cilia J, Gartlon JE, Jones DN (2007). "Effect of the selective dopamine D3 receptor antagonist SB-277011-A on regional c-Fos-like expression in rat forebrain". Brain research 1149: 50–7. PMID 17382304. doi:10.1016/j.brainres.2007.02.051. 
  6. Reavill C, Taylor SG, Wood MD, Ashmeade T, Austin NE, Avenell KY, Boyfield I, Branch CL, Cilia J (2000). "Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A". The Journal of pharmacology and experimental therapeutics 294 (3): 1154–65. PMID 10945872. 
  7. Le Foll B, Schwartz JC, Sokoloff P (2003). "Disruption of nicotine conditioning by dopamine D(3) receptor ligands". Molecular psychiatry 8 (2): 225–30. PMID 12610655. doi:10.1038/sj.mp.4001202. 
  8. Vorel SR, Ashby Jr CR, Paul M, Liu X, Hayes R, Hagan JJ, Middlemiss DN, Stemp G, Gardner EL (2002). "Dopamine D3 receptor antagonism inhibits cocaine-seeking and cocaine-enhanced brain reward in rats". Journal of Neuroscience 22 (21): 9595–603. PMID 12417684. 
  9. Di Ciano P, Underwood RJ, Hagan JJ Everitt BJ (2003). "Attenuation of cue-controlled cocaine-seeking by a selective D3 dopamine receptor antagonist SB-277011-A". Neuropsychopharmacology 28 (2): 329–38. PMID 12589386. doi:10.1038/sj.npp.1300148. 

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