6'-(3-氯苄基氧基)-3,4,5,6-四氢-2H-[1,2']联吡嗪

• 常用名: 6'-(3-氯苄基氧基)-3,4,5,6-四氢-2H-[1,2']联吡嗪
• 英文名: CP-809101
• CAS号: 479683-64-2
• 分子量: 304.77
• 密度: 1.3±0.1 g/cm3
• 沸点: 486.6±45.0 °C at 760 mmHg
• 分子式: C₁₅H₁₇ClN₄O
• 熔点: N/A
• 闪点: 248.1±28.7 °C

用途

CP-809101是5-HT2C受体激动剂，对人5-HT2C，5-HT2B和5-HT2A受体的pEC50分别为9.96，7.19和6.81。

名称

• 中文名: 6'-(3-氯苄基氧基)-3,4,5,6-四氢-2H-[1,2']联吡嗪
• 英文名: 2-[(3-chlorophenyl)methoxy]-6-piperazin-1-ylpyrazine

生物活性

• 描述: CP-809101是5-HT2C受体激动剂,对人5-HT2C,5-HT2B和5-HT2A受体的pEC50分别为9.96,7.19和6.81。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体
  信号通路 >> 神经信号通路 >> 5-HT受体
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Higgins GA, Silenieks LB, Lau W, et al. Evaluation of chemically diverse 5-HT2C receptor agonists on behaviours motivated by food and nicotine and on side effect profiles. Psychopharmacology (Berl). 2013 Apr;226(3):475-90.

  [2]. Strong PV, Christianson JP, Loughridge AB, et al. 5-hydroxytryptamine 2C receptors in the dorsal striatum mediate stress-induced interference with negatively reinforced instrumental escape behavior. Neuroscience. 2011 Dec 1;197:132-44. doi: 10.1016/j.neur

  [3]. Fletcher PJ, Tampakeras M, Sinyard J et al. Characterizing the effects of 5-HT(2C) receptor ligands on motor activity and feeding behaviour in 5-HT(2C) receptor knockout mice. Neuropharmacology. 2009 Sep;57(3):259-67. doi: 10.1016/j.neuropharm.2009.05.011

  [4]. Siuciak JA, Chapin DS, McCarthy SA, et al. CP-809,101, a selective 5-HT2C agonist, shows activity in animal models of antipsychotic activity. Neuropharmacology. 2007 Feb;52(2):279-90.

物理化学性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 486.6±45.0 °C at 760 mmHg
• 分子式: C₁₅H₁₇ClN₄O
• 分子量: 304.77
• 闪点: 248.1±28.7 °C
• PSA: 50.28000
• LogP: 3.02
• InChIKey: PCWGGOVOEWHPMG-UHFFFAOYSA-N
• SMILES: Clc1cccc(COc2cncc(N3CCNCC3)n2)c1
• 蒸汽压: 0.0±1.2 mmHg at 25°C
• 折射率: 1.597
• 储存条件: 2-8℃

靶点实验

查看更多实验

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

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：Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumu... 来源：ChEMBL 靶标：5-hydroxytryptamine receptor 2A External Id：CHEMBL2342580

实验名称：Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumu... 来源：ChEMBL 靶标：5-hydroxytryptamine receptor 2C External Id：CHEMBL2342579

实验名称：Metabolic stability in human liver microsomes in presence of CYP1A2 inhibitor furafyl... 来源：ChEMBL 靶标：Liver microsomes External Id：CHEMBL1021501

实验名称：Binding affinity to 5-HT2C receptor 来源：ChEMBL 靶标：5-hydroxytryptamine receptor 2C External Id：CHEMBL1040388

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

实验名称：Cytochrome P450 family 3 subfamily A member 7 (CYP3A7) small molecule antagonists: lu... 来源：NCGC External Id：CYP3A7681

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英文别名

• 2-[(3-Chlorobenzyl)oxy]-6-(1-piperazinyl)pyrazine
• cs-1201
• CP-809,101
• CP-809101