SB-277011-A
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]
(IUPAC) ime | |||
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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 | ||
Hemijski podaci | |||
Formula | C28H30N4O | ||
Mol. masa | 438,563 g/mol | ||
SMILES | eMolekuli & PubHem | ||
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Farmakoinformacioni podaci | |||
Trudnoća | ? | ||
Pravni status |
SB-277,011A se koristi za studiranje adikcije na stimulišuće droge poput nikotina[7] i kokaina.[8][9]
Reference uredi
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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. DOI:10.1021/jm000090i. PMID 10794704.
- ↑ 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. DOI:10.1016/j.brainres.2007.02.051. PMID 17382304.
- ↑ 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.
- ↑ Le Foll B, Schwartz JC, Sokoloff P (2003). „Disruption of nicotine conditioning by dopamine D(3) receptor ligands”. Molecular psychiatry 8 (2): 225–30. DOI:10.1038/sj.mp.4001202. PMID 12610655.
- ↑ 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.
- ↑ 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. DOI:10.1038/sj.npp.1300148. PMID 12589386.