Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

SB-277,011-A

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
SB-277,011-A
Identifiers
  • N-{trans-4-[2-(6-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl]cyclohexyl}quinoline-4-carboxamide
CAS Number
PubChemCID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC28H30N4O
Molar mass438.575 g·mol−1
3D model (JSmol)
  • c4cccc1c4nccc1C(=O)NC3CCC(CC3)CCN(CCc2c5)Cc2ccc5C#N
  • InChI=1S/C28H30N4O/c29-18-21-5-8-23-19-32(16-13-22(23)17-21)15-12-20-6-9-24(10-7-20)31-28(33)26-11-14-30-27-4-2-1-3-25(26)27/h1-5,8,11,14,17,20,24H,6-7,9-10,12-13,15-16,19H2,(H,31,33) ☒N
  • Key:OLWRVVHPJFLNPW-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

SB-277,011A is a drug which acts as a potent and selectivedopamineD3 receptorantagonist,[1] which is around 80–100 times selective for D3 over D2,[2] and lacks anypartial agonist activity.[3]

SB-277,011A is used in the study ofaddiction tostimulant drugs such asnicotine[4] andcocaine.[5][6] Where cocaine reduces the threshold for brain electrical self-stimulation in rats, an indication of cocaine'srewarding 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 toheroin[10] andalcohol.[11][12][13]

Another potential application for SB-277,011A is in the treatment ofschizophrenia,[14] and it may be particularly useful in treatingcomorbid patients who are both schizophrenic and addicted to drugs.[15] However it may worsen side effects such astardive dyskinesia in patients who are already prescribedantipsychotic drugs.[16]

See also

[edit]

References

[edit]
  1. ^Stemp G, Ashmeade T, Branch CL, Hadley MS, Hunter AJ, Johnson CN, et al. (May 2000). "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.doi:10.1021/jm000090i.PMID 10794704.
  2. ^Southam E, Lloyd A, Jennings CA, Cluderay JE, Cilia J, Gartlon JE, Jones DN (May 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.S2CID 12557234.
  3. ^Reavill C, Taylor SG, Wood MD, Ashmeade T, Austin NE, Avenell KY, et al. (September 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 (February 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 CR, Paul M, Liu X, Hayes R, Hagan JJ, et al. (November 2002)."Dopamine D3 receptor antagonism inhibits cocaine-seeking and cocaine-enhanced brain reward in rats".The Journal of Neuroscience.22 (21):9595–603.doi:10.1523/JNEUROSCI.22-21-09595.2002.PMC 6758043.PMID 12417684.
  6. ^Di Ciano P, Underwood RJ, Hagan JJ, Everitt BJ (February 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 (July 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 (March 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 CR, Hagan JJ, et al. (October 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.PMC 3726040.PMID 15083257.
  10. ^Ashby CR, Paul M, Gardner EL, Heidbreder CA, Hagan JJ (June 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.S2CID 26458149.
  11. ^Thanos PK, Katana JM, Ashby CR, Michaelides M, Gardner EL, Heidbreder CA, Volkow ND (May 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.S2CID 15406751.
  12. ^Vengeliene V, Leonardi-Essmann F, Perreau-Lenz S, Gebicke-Haerter P, Drescher K, Gross G, Spanagel R (November 2006)."The dopamine D3 receptor plays an essential role in alcohol-seeking and relapse".FASEB Journal.20 (13):2223–33.doi:10.1096/fj.06-6110com.PMID 17077299.S2CID 9431585.
  13. ^Heidbreder CA, Andreoli M, Marcon C, Hutcheson DM, Gardner EL, Ashby CR (March 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.S2CID 25984106.
  14. ^Joyce JN, Millan MJ (July 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 (January 2008). "Experimental pharmacotherapeutics for schizophrenia and addiction".IDrugs.11 (1):7–9.PMID 18175251.
  16. ^Malik P, Andersen MB, Peacock L (August 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.S2CID 19410897.
D1-like
Agonists
PAMs
Antagonists
D2-like
Agonists
Antagonists
Retrieved from "https://en.wikipedia.org/w/index.php?title=SB-277,011-A&oldid=1255735373"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2025 Movatter.jp