Chemistry:SB-277,011-A
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Short description: Chemical compound
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| Formula | C28H30N4O |
| Molar mass | 438.575 g·mol−1 |
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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]
References
- ↑ "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 43 (9): 1878–85. May 2000. doi:10.1021/jm000090i. PMID 10794704.
- ↑ "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. May 2007. doi:10.1016/j.brainres.2007.02.051. PMID 17382304.
- ↑ "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. September 2000. PMID 10945872.
- ↑ "Disruption of nicotine conditioning by dopamine D(3) receptor ligands". Molecular Psychiatry 8 (2): 225–30. February 2003. doi:10.1038/sj.mp.4001202. PMID 12610655.
- ↑ "Dopamine D3 receptor antagonism inhibits cocaine-seeking and cocaine-enhanced brain reward in rats". The Journal of Neuroscience 22 (21): 9595–603. November 2002. doi:10.1523/JNEUROSCI.22-21-09595.2002. PMID 12417684.
- ↑ "Attenuation of cue-controlled cocaine-seeking by a selective D3 dopamine receptor antagonist SB-277011-A". Neuropsychopharmacology 28 (2): 329–38. February 2003. doi:10.1038/sj.npp.1300148. PMID 12589386.
- ↑ "Selective antagonism at dopamine D3 receptors prevents nicotine-triggered relapse to nicotine-seeking behavior". Neuropsychopharmacology 28 (7): 1272–80. July 2003. doi:10.1038/sj.npp.1300183. PMID 12700694.
- ↑ "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. March 2007. doi:10.1016/j.ejphar.2007.01.004. PMID 17303116.
- ↑ "Blockade of mesolimbic dopamine D3 receptors inhibits stress-induced reinstatement of cocaine-seeking in rats". Psychopharmacology 176 (1): 57–65. October 2004. doi:10.1007/s00213-004-1858-y. PMID 15083257.
- ↑ "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. June 2003. doi:10.1002/syn.10188. PMID 12645041.
- ↑ "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. May 2005. doi:10.1016/j.pbb.2005.03.013. PMID 15894078.
- ↑ "The dopamine D3 receptor plays an essential role in alcohol-seeking and relapse". FASEB Journal 20 (13): 2223–33. November 2006. doi:10.1096/fj.06-6110com. PMID 17077299.
- ↑ "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. March 2007. doi:10.1111/j.1369-1600.2007.00051.x. PMID 17407496.
- ↑ "Dopamine D3 receptor antagonists as therapeutic agents". Drug Discovery Today 10 (13): 917–25. July 2005. doi:10.1016/S1359-6446(05)03491-4. PMID 15993811.
- ↑ "Experimental pharmacotherapeutics for schizophrenia and addiction". IDrugs 11 (1): 7–9. January 2008. PMID 18175251.
- ↑ "The effects of dopamine D3 agonists and antagonists in a nonhuman primate model of tardive dyskinesia". Pharmacology, Biochemistry, and Behavior 78 (4): 805–10. August 2004. doi:10.1016/j.pbb.2004.05.019. PMID 15301939.
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