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
• InChIKey: OLWRVVHPJFLNPW-UHFFFAOYSA-N
• SMILES: N#Cc1ccc2c(c1)CCN(CCC1CCC(NC(=O)c3ccnc4ccccc34)CC1)C2
• 蒸汽压: 0.0±2.1 mmHg at 25°C
• 折射率: 1.656
• 储存条件: 2-8℃

靶点实验

查看更多实验

实验名称：Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293 cel... 来源：ChEMBL 靶标：D(2) dopamine receptor External Id：CHEMBL4053560

实验名称：NCATS Kinetic Aqueous Solubility Profiling 来源：NCGC 靶标：N/A External Id：ADME-solubility1

实验名称：Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293 cell... 来源：ChEMBL 靶标：D(3) dopamine receptor External Id：CHEMBL4053561

实验名称：Primary qHTS assay for small molecule inhibitors of Inositol hexaphosphate kinase 1 (... 来源：NCGC External Id：IP6K1-p1

实验名称：Competitive antagonist activity at D3 receptor (unknown origin) expressed in CHOK1 ce... 来源：ChEMBL 靶标：D(3) dopamine receptor External Id：CHEMBL4053559

实验名称：Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: lu... 来源：NCGC External Id：CYP3A4437

实验名称：Agonist activity at D2 long receptor (unknown origin) expressed in CHOK1 cells assess... 来源：ChEMBL 靶标：D(2) dopamine receptor External Id：CHEMBL4053568

实验名称：Cytochrome P450 family 2 subfamily D member 6 (CYP2D6) small molecule antagonists: lu... 来源：NCGC External Id：CYP2D6395

实验名称：Agonist activity at D3 receptor (unknown origin) expressed in CHOK1 cells assessed as... 来源：ChEMBL 靶标：D(3) dopamine receptor External Id：CHEMBL4053569

实验名称：Antagonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS bin... 来源：ChEMBL 靶标：D(2) dopamine receptor External Id：CHEMBL1059864

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英文别名

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