SB-277,011-A

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SB-277,011-A
SB2770112DACS.svg
Systematic (IUPAC) name
N-{trans-4-[2-(6-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl]cyclohexyl}quinoline-4-carboxamide
Identifiers
PubChem CID: 5311096
IUPHAR/BPS 143
ChEMBL CHEMBL85606 N
Chemical data
Formula C28H30N4O
Molecular mass 438.563 g/mol
  • c4cccc1c4nccc1C(=O)NC3CCC(CC3)CCN(CCc2c5)Cc2ccc5C#N
 NYesY (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]

References

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  10. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  11. ↑ Lua error in package.lua at line 80: module 'strict' not found.
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  14. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  15. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  16. ↑ Lua error in package.lua at line 80: module 'strict' not found.
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