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{{Drugbox | verifiedrevid = 447993852 | IUPAC_name = N-{trans-4-cyclohexyl}quinoline-4-carboxamide | image = SB277011A.png | width = 260

| tradename = | legal_status = | routes_of_administration =

| metabolism = | elimination_half-life = | excretion =

| CAS_number = | PubChem = 5311096 | IUPHAR_ligand = 143 | DrugBank_Ref =

| C=28 | H=30 | N=4 | O=1 | molecular_weight = 438.563 g/mol | smiles = c4cccc1c4nccc1C(=O)NC3CCC(CC3)CCN(CCc2c5)Cc2ccc5C#N }}

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

SB-277,011A is used in the study of addiction to stimulant drugs such as nicotine and cocaine. 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, and is also being investigated for potential uses in the treatment of other drug addictions, such as addiction to heroin and alcohol.

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

References

1. 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.
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. doi:10.1016/j.brainres.2007.02.051. PMID 17382304.
3. 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.
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. doi:10.1038/sj.mp.4001202. PMID 12610655.
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. doi:10.1038/sj.npp.1300148. PMID 12589386.
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. doi:10.1038/sj.npp.1300183. PMID 12700694.
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. doi:10.1016/j.ejphar.2007.01.004. PMID 17303116.
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. doi:10.1007/s00213-004-1858-y. PMID 15083257.
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. doi:10.1002/syn.10188. PMID 12645041.
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. doi:10.1016/j.pbb.2005.03.013. PMID 15894078.
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. doi:10.1096/fj.06-6110com. PMID 17077299.{{cite journal}}: CS1 maint: unflagged free DOI (link)
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. doi:10.1111/j.1369-1600.2007.00051.x. PMID 17407496.
14. Joyce, JN; Millan, MJ (2005). "Dopamine D3 receptor antagonists as therapeutic agents". Drug discovery today. 10 (13): 917–25. doi:10.1016/S1359-6446(05)03491-4. PMID 15993811.
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. doi:10.1016/j.pbb.2004.05.019. PMID 15301939.

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