SB-277,011-A (original) (raw)
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.
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| dbo:abstract | 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. (en) SB-277,011A é uma droga que actua como um potente e selectivo antagonista do receptor D3 de dopamina, e que é 80-100x selectivo para o receptor D3 em relação ao D2, e faltando-lhe qualquer actividade de agonista parcial. SB-277,011A é usado no estudo da adicção de drogas estimulantes como a nicotina. e a cocaína. Onde a cocaína reduz o limite de auto-estimulação eléctrica do cérebro em ratos, uma indicação dos efeitos de recompensa da cocaína, o SB-277,011A reverte completamente este efeito. Pode então ser útil no tratamento da adicção a nicotina e cocaína, e também está a ser investigado o potencial uso no tratamento de outras adicções de drogas, como a de heroína e de álcool. Outra possível aplicação do SB-277,011A é no tratamento da esquizofrenia, e pode ser particularmente útil no tratamento de doentes comórbidos, que são simultaneamente esquizofrénicos e adictos a drogas. No entanto, poderá piorar efeitos secundários como a discinesia tardia em doentes a quem foram já prescritas drogas antipsicóticas. (pt) |
| dbo:chEMBL | 85606 |
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| dbp:iupacName | N-{trans-4-[2-ethyl]cyclohexyl}quinoline-4-carboxamide (en) |
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| dbp:smiles | c4cccc1c4nccc1CNC3CCCCCNCc2ccc5C#N (en) |
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| dcterms:subject | dbc:D3_antagonists dbc:Benzonitriles dbc:Carboxamides dbc:Quinolines dbc:Tetrahydroisoquinolines |
| gold:hypernym | dbr:Drug |
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| rdfs:comment | 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. (en) SB-277,011A é uma droga que actua como um potente e selectivo antagonista do receptor D3 de dopamina, e que é 80-100x selectivo para o receptor D3 em relação ao D2, e faltando-lhe qualquer actividade de agonista parcial. Outra possível aplicação do SB-277,011A é no tratamento da esquizofrenia, e pode ser particularmente útil no tratamento de doentes comórbidos, que são simultaneamente esquizofrénicos e adictos a drogas. No entanto, poderá piorar efeitos secundários como a discinesia tardia em doentes a quem foram já prescritas drogas antipsicóticas. (pt) |
| rdfs:label | SB-277,011-A (en) SB-277011-A (pt) |
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