N-((1r,4r)-4-(2-(6-氰基-3,4-二氢异喹啉-2(1h)-基)乙基)环己基)喹啉-4-羧酰胺

• 常用名: N-((1r,4r)-4-(2-(6-氰基-3,4-二氢异喹啉-2(1h)-基)乙基)环己基)喹啉-4-羧酰胺
• 英文名: SB-277011
• CAS号: 215803-78-4
• 分子量: 438.564
• 密度: 1.2±0.1 g/cm3
• 沸点: 679.3±55.0 °C at 760 mmHg
• 分子式: C₂₈H₃₀N₄O
• 熔点: N/A
• 闪点: 364.6±31.5 °C

用途

SB-277011是可渗透入脑的多巴胺D3受体拮抗剂,对D3,D2,5-HT1D和5-HT1B的pKi分别为8.0,6.0,5.0和<5.2。

名称

• 中文名: N-((1r,4r)-4-(2-(6-氰基-3,4-二氢异喹啉-2(1h)-基)乙基)环己基)喹啉-4-羧酰胺
• 英文名: N-[4-[2-(6-cyano-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]cyclohexyl]quinoline-4-carboxamide

生物活性

• 描述: SB-277011是可渗透入脑的多巴胺D3受体拮抗剂,对D3,D2,5-HT1D和5-HT1B的pKi分别为8.0,6.0,5.0和<5.2。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体
  信号通路 >> 神经信号通路 >> 多巴胺受体
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Clément P, Pozzato C, Heidbreder C, Alexandre L, Giuliano F, Melotto S.Delay of ejaculation induced by SB-277011, a selective dopamine D3 receptor antagonist, in the rat.J Sex Med. 2009 Apr;6(4):980-8. Epub 2008 Feb 4.

  [2]. Gyertyán I, Sághy K.The selective dopamine D3 receptor antagonists, SB 277011-A and S 33084 block haloperidol-induced catalepsy in rats.Eur J Pharmacol. 2007 Oct 31;572(2-3):171-4. Epub 2007 Jun 29.

  [3]. Southam E, Lloyd A, Jennings CA, Cluderay JE, Cilia J, Gartlon JE, Jones DN.Effect of the selective dopamine D3 receptor antagonist SB-277011-A on regional c-Fos-like expression in rat forebrain.Brain Res. 2007 May 29;1149:50-7. Epub 2007 Feb 28.

  [4]. Pak AC, Ashby CR Jr, Heidbreder CA, Pilla M, Gilbert J, Xi ZX, Gardner EL.The selective dopamine D3 receptor antagonist SB-277011A reduces nicotine-enhanced brain reward and nicotine-paired environmental cue functions.Int J Neuropsychopharmacol. 2006 Oct;

  [5]. Higley, Amanda E.; Kiefer, Stephen W.; Li, Xia; Gaal, Jozsef; Xi, Zheng-Xiong; Gardner, Eliot L. Dopamine D3 receptor antagonist SB-277011A inhibits methamphetamine self-administration and methamphetamine-induced reinstatement of drug-seeking in rats. Eur

物理化学性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 679.3±55.0 °C at 760 mmHg
• 分子式: C₂₈H₃₀N₄O
• 分子量: 438.564
• 闪点: 364.6±31.5 °C
• 精确质量: 438.241974
• PSA: 69.02000
• LogP: 4.26
• 蒸汽压: 0.0±2.1 mmHg at 25°C
• 折射率: 1.656
• 储存条件: 2-8℃

英文别名

• N-{trans-4-[2-(6-Cyano-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]cyclohexyl}-4-quinolinecarboxamide
• cc-478
• 4-Quinolinecarboxamide, N-[trans-4-[2-(6-cyano-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]cyclohexyl]-
• N-{trans-4-[2-(6-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl]cyclohexyl}quinoline-4-carboxamide
• SB-277011