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SB-277,011-A: Wikis


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Systematic (IUPAC) name
ATC code  ?
PubChem 5311096
Chemical data
Formula C28H30N4O 
Mol. mass 438.563 g/mol
SMILES eMolecules & PubChem
Therapeutic considerations
Pregnancy cat.  ?
Legal status

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, Vong AK, Austin NE, Jeffrey P, Avenell KY, Boyfield I, Hagan JJ, Middlemiss DN, Reavill C, Riley GJ, Routledge C, Wood M. Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-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. 2000 May 4;43(9):1878-85. PMID 10794704
  2. ^ Southam E, Lloyd A, Jennings CA, Cluderay JE, Cilia J, Gartlon JE, Jones DN. Effect of the selective dopamine D3 receptor antagonist SB-277011-A on regional c-Fos-like expression in rat forebrain. Brain Research. 2007 May 29;1149:50-7. PMID 17382304
  3. ^ Reavill C, Taylor SG, Wood MD, Ashmeade T, Austin NE, Avenell KY, Boyfield I, Branch CL, Cilia J, Coldwell MC, Hadley MS, Hunter AJ, Jeffrey P, Jewitt F, Johnson CN, Jones DN, Medhurst AD, Middlemiss DN, Nash DJ, Riley GJ, Routledge C, Stemp G, Thewlis KM, Trail B, Vong AK, Hagan JJ. Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A. Journal of Pharmacology and Experimental Therapeutics. 2000 Sep;294(3):1154-65. PMID 10945872
  4. ^ Le Foll B, Schwartz JC, Sokoloff P. Disruption of nicotine conditioning by dopamine D(3) receptor ligands. Molecular Psychiatry. 2003 Feb;8(2):225-30. PMID 12610655
  5. ^ Vorel SR, Ashby CR Jr, Paul M, Liu X, Hayes R, Hagan JJ, Middlemiss DN, Stemp G, Gardner EL. Dopamine D3 receptor antagonism inhibits cocaine-seeking and cocaine-enhanced brain reward in rats. Journal of Neuroscience. 2002 Nov 1;22(21):9595-603. PMID 12417684
  6. ^ Di Ciano P, Underwood RJ, Hagan JJ, Everitt BJ. Attenuation of cue-controlled cocaine-seeking by a selective D3 dopamine receptor antagonist SB-277011-A. Neuropsychopharmacology. 2003 Feb;28(2):329-38. PMID 12589386
  7. ^ Andreoli M, Tessari M, Pilla M, Valerio E, Hagan JJ, Heidbreder CA. Selective antagonism at dopamine D3 receptors prevents nicotine-triggered relapse to nicotine-seeking behavior. Neuropsychopharmacology. 2003 Jul;28(7):1272-80. PMID 12700694
  8. ^ Ross JT, Corrigall WA, Heidbreder CA, LeSage MG. 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. 2007 Mar 22;559(2-3):173-9. PMID 17303116
  9. ^ Xi ZX, Gilbert J, Campos AC, Kline N, Ashby CR Jr, Hagan JJ, Heidbreder CA, Gardner EL. Blockade of mesolimbic dopamine D3 receptors inhibits stress-induced reinstatement of cocaine-seeking in rats. Psychopharmacology (Berlin). 2004 Oct;176(1):57-65. PMID 15083257
  10. ^ Ashby CR Jr, Paul M, Gardner EL, Heidbreder CA, Hagan JJ. 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. 2003 Jun 1;48(3):154-6. PMID 12645041
  11. ^ Thanos PK, Katana JM, Ashby CR Jr, Michaelides M, Gardner EL, Heidbreder CA, Volkow ND. The selective dopamine D3 receptor antagonist SB-277011-A attenuates ethanol consumption in ethanol preferring (P) and non-preferring (NP) rats. Pharmacology, Biochemistry and Behaviour. 2005 May;81(1):190-7. PMID 15894078
  12. ^ Vengeliene V, Leonardi-Essmann F, Perreau-Lenz S, Gebicke-Haerter P, Drescher K, Gross G, Spanagel R. The dopamine D3 receptor plays an essential role in alcohol-seeking and relapse. FASEB Journal. 2006 Nov;20(13):2223-33. PMID 17077299
  13. ^ Heidbreder CA, Andreoli M, Marcon C, Hutcheson DM, Gardner EL, Ashby CR Jr. Evidence for the role of dopamine D3 receptors in oral operant alcohol self-administration and reinstatement of alcohol-seeking behavior in mice. Addiction Biology. 2007 Mar;12(1):35-50. PMID 17407496
  14. ^ Joyce JN, Millan MJ. Dopamine D3 receptor antagonists as therapeutic agents. Drug Discovery Today. 2005 Jul 1;10(13):917-25. PMID 15993811
  15. ^ Jahnke U. Experimental pharmacotherapeutics for schizophrenia and addiction. IDrugs. 2008 Jan;11(1):7-9. PMID 18175251
  16. ^ Malik P, Andersen MB, Peacock L. The effects of dopamine D3 agonists and antagonists in a nonhuman primate model of tardive dyskinesia. Pharmacology, Biochemistry and Behaviour. 2004 Aug;78(4):805-10. PMID 15301939


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