S1RA

• 常用名: S1RA
• 英文名: S1RA
• CAS号: 878141-96-9
• 分子量: 337.415
• 密度: 1.2±0.1 g/cm3
• 沸点: 528.1±50.0 °C at 760 mmHg
• 分子式: C₂₀H₂₃N₃O₂
• 熔点: N/A
• 闪点: 273.2±30.1 °C

S1RA用途

S1RA(E-52862)是高活性和选择性的sigma-1受体(σ1R)拮抗剂,Ki为17nM,而对σ2R的Ki则高于1000nM。

S1RA名称

• 中文名: S1RA
• 英文名: 4-(2-{[5-Methyl-1-(2-naphthyl)-1H-pyrazol-3-yl]oxy}ethyl)morpholi ne

S1RA生物活性

• 描述: S1RA(E-52862)是高活性和选择性的sigma-1受体(σ1R)拮抗剂,Ki为17nM,而对σ2R的Ki则高于1000nM。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> Sigma Receptor
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Díaz JL, et al. Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862). J Med Chem. 2012 Oct 11;55(19):8211-24.

  [2]. Romero L, et al. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. Br J Pharmacol. 2012 Aug;166(8):2289-306.

  [3]. Vidal-Torres A, et al. Effects of the selective sigma-1 receptor antagonist S1RA on formalin-induced pain behavior and neurotransmitter release in the spinal cord in rats. J Neurochem. 2014 Jan 3.

S1RA物理化学性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 528.1±50.0 °C at 760 mmHg
• 分子式: C₂₀H₂₃N₃O₂
• 分子量: 337.415
• 闪点: 273.2±30.1 °C
• 精确质量: 337.179016
• PSA: 39.52000
• LogP: 3.37
• InChIKey: DGPGXHRHNRYVDH-UHFFFAOYSA-N
• SMILES: Cc1cc(OCCN2CCOCC2)nn1-c1ccc2ccccc2c1
• 外观性状: 白色至类白色固体
• 蒸汽压: 0.0±1.4 mmHg at 25°C
• 折射率: 1.621
• 储存条件: -20℃

S1RA靶点实验

查看更多实验

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：Antinociceptive activity in CD1 mouse assessed as reduction of capsaicin-induced mech... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4262377

实验名称：Antinociceptive activity in CD1 mouse assessed as reduction of capsaicin-induced mech... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4262376

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

实验名称：Displacement of [3H]-(+)-pentazocine from recombinant human sigma1 receptor expressed... 来源：ChEMBL 靶标：Sigma non-opioid intracellular receptor 1 External Id：CHEMBL4262391

实验名称：Cytochrome P450 family 2 subfamily C member 9 (CYP2C9) small molecule antagonists: lu... 来源：NCGC External Id：CYP2C9536

实验名称：Antinociceptive activity in CD1 mouse partial sciatic nerve ligation model assessed a... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4262367

实验名称：Antinociceptive activity in formalin-induced nociceptive CD1 mouse model assessed as ... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4262361

实验名称：Antinociceptive activity in formalin-induced nociceptive CD1 mouse model assessed as ... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL4262360

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S1RA英文别名

• 4-(2-{[5-Methyl-1-(2-naphthyl)-1H-pyrazol-3-yl]oxy}ethyl)morpholine
• E-52862
• S1RA