SB-277,011-A

SB-277,011A is a drug which acts as a potent and selective dopamine D₃ receptor antagonist,^[1] which is around 80–100 times selective for D₃ over D₂,^[2] and lacks any partial agonist activity.^[3]

SB-277,011-A

Identifiers
IUPAC name N-{trans-4-[2-(6-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl]cyclohexyl}quinoline-4-carboxamide
CAS Number	215803-78-4 N[EPA]
PubChem CID	5311096
IUPHAR/BPS	143
ChemSpider	4470626 N
UNII	CHW57ND47C
ChEMBL	ChEMBL85606 N
CompTox Dashboard (EPA)	DTXSID10944188
Chemical and physical data
Formula	C28H30N4O
Molar mass	438.575 g·mol−1
3D model (JSmol)	Interactive image
SMILES c4cccc1c4nccc1C(=O)NC3CCC(CC3)CCN(CCc2c5)Cc2ccc5C#N
InChI 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
NY (what is this?)  (verify)

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]

See also

• GSK-598809
• Nafadotride
• PNU-99,194