Open Access Articles- Top Results for SB-277,011-A


Systematic (IUPAC) name
Clinical data
PubChem CID 5311096
IUPHAR ligand 143
Chemical data
Formula C28H30N4O
438.563 g/mol
 14pxN (what is this?)  (verify)

SB-277,011A is a drug which acts as a potent and selective dopamine D3 receptor antagonist,[1] which is around 80-100x selective for D3 over D2,[2] and lacks any partial agonist activity.[3]

SB-277,011A is used in the study of addiction to stimulant drugs such as nicotine[4] and cocaine.[5][6] Where cocaine reduces the threshold for brain electrical self-stimulation in rats, an indication of cocaine's rewarding effects, SB-277,011A completely reverses this effect. It may thus be useful in the treatment of addiction to nicotine and cocaine,[7][8][9] and is also being investigated for potential uses in the treatment of other drug addictions, such as addiction to heroin[10] and alcohol.[11][12][13]

Another potential application for SB-277,011A is in the treatment of schizophrenia,[14] and it may be particularly useful in treating comorbid patients who are both schizophrenic and addicted to drugs.[15] However it may worsen side effects such as tardive dyskinesia in patients who are already prescribed antipsychotic drugs.[16]


  1. ^ Stemp, G; Ashmeade, T; Branch, CL; Hadley, MS; Hunter, AJ; Johnson, CN; Nash, DJ; Thewlis, KM et al. (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 Medical Chemistry 43 (9): 1878–85. PMID 10794704. doi:10.1021/jm000090i. 
  2. ^ 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. 
  3. ^ Reavill, C; Taylor, SG; Wood, MD; Ashmeade, T; Austin, NE; Avenell, KY; Boyfield, I; Branch, CL et al. (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. 
  4. ^ 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/ 
  5. ^ 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. 
  6. ^ 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. 
  7. ^ Andreoli, M; Tessari, M; Pilla, M; Valerio, E; Hagan, JJ; Heidbreder, CA (2003). "Selective antagonism at dopamine D3 receptors prevents nicotine-triggered relapse to nicotine-seeking behavior". Neuropsychopharmacology 28 (7): 1272–80. PMID 12700694. doi:10.1038/sj.npp.1300183. 
  8. ^ Ross, JT; Corrigall, WA; Heidbreder, CA; Lesage, MG (2007). "Effects of the selective dopamine D3 receptor antagonist SB-277011A on the reinforcing effects of nicotine as measured by a progressive-ratio schedule in rats". European Journal of Pharmacology 559 (2–3): 173–9. PMID 17303116. doi:10.1016/j.ejphar.2007.01.004. 
  9. ^ Xi, ZX; Gilbert, J; Campos, AC; Kline, N; Ashby Jr, CR; Hagan, JJ; Heidbreder, CA; Gardner, EL (2004). "Blockade of mesolimbic dopamine D3 receptors inhibits stress-induced reinstatement of cocaine-seeking in rats". Psychopharmacology 176 (1): 57–65. PMID 15083257. doi:10.1007/s00213-004-1858-y. 
  10. ^ Ashby Jr, CR; Paul, M; Gardner, EL; Heidbreder, CA; Hagan, JJ (2003). "Acute administration of the selective D3 receptor antagonist SB-277011A blocks the acquisition and expression of the conditioned place preference response to heroin in male rats". Synapse 48 (3): 154–6. PMID 12645041. doi:10.1002/syn.10188. 
  11. ^ Thanos, PK; Katana, JM; Ashby Jr, CR; Michaelides, M; Gardner, EL; Heidbreder, CA; Volkow, ND (2005). "The selective dopamine D3 receptor antagonist SB-277011-A attenuates ethanol consumption in ethanol preferring (P) and non-preferring (NP) rats". Pharmacology, Biochemistry, and Behavior 81 (1): 190–7. PMID 15894078. doi:10.1016/j.pbb.2005.03.013. 
  12. ^ Vengeliene, V; Leonardi-Essmann, F; Perreau-Lenz, S; Gebicke-Haerter, P; Drescher, K; Gross, G; Spanagel, R (2006). "The dopamine D3 receptor plays an essential role in alcohol-seeking and relapse". The FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20 (13): 2223–33. PMID 17077299. doi:10.1096/fj.06-6110com. 
  13. ^ Heidbreder, CA; Andreoli, M; Marcon, C; Hutcheson, DM; Gardner, EL; Ashby Jr, CR (2007). "Evidence for the role of dopamine D3 receptors in oral operant alcohol self-administration and reinstatement of alcohol-seeking behavior in mice". Addiction biology 12 (1): 35–50. PMID 17407496. doi:10.1111/j.1369-1600.2007.00051.x. 
  14. ^ Joyce, JN; Millan, MJ (2005). "Dopamine D3 receptor antagonists as therapeutic agents". Drug Discovery Today 10 (13): 917–25. PMID 15993811. doi:10.1016/S1359-6446(05)03491-4. 
  15. ^ Jahnke, U (2008). "Experimental pharmacotherapeutics for schizophrenia and addiction". IDrugs : the investigational drugs journal 11 (1): 7–9. PMID 18175251. 
  16. ^ Malik, P; Andersen, MB; Peacock, L (2004). "The effects of dopamine D3 agonists and antagonists in a nonhuman primate model of tardive dyskinesia". Pharmacology, Biochemistry, and Behavior 78 (4): 805–10. PMID 15301939. doi:10.1016/j.pbb.2004.05.019. 

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