Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1R,2R,5S,6R)-rel- (9CI)

• 常用名: Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1R,2R,5S,6R)-rel- (9CI)
• 英文名: Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1R,2R,5S,6R)-rel- (9CI)
• CAS号: 176027-90-0
• 分子量: 185.18
• 密度: 1.6±0.1 g/cm3
• 沸点: 376.4±32.0 °C at 760 mmHg
• 分子式: C₈H₁₁NO₄
• 熔点: N/A
• 闪点: 181.4±25.1 °C

用途

(rel)-Eglumegad((rel,LY354740)是Eglumegad(HY-18941)的外消旋异构体。Eglumegad是一种高效和选择性的II组(mGlu2/3)受体激动剂,对转染的人mGlu2和mGlu3受体的EC50分别为5和24nM[1]。

名称

• 英文名: Eglumetad

生物活性

• 描述: (rel)-Eglumegad((rel,LY354740)是Eglumegad(HY-18941)的外消旋异构体。Eglumegad是一种高效和选择性的II组(mGlu2/3)受体激动剂,对转染的人mGlu2和mGlu3受体的EC50分别为5和24nM[1]。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 谷氨酸受体
  研究领域 >> 神经疾病
• 靶点实验:

  mGluR2[1]

• 参考文献:

  [1]. Boerner T, et al. The group II metabotropic glutamate receptor agonist LY354740 and the D2 receptor antagonist haloperidol reduce locomotor hyperactivity but fail to rescue spatial working memory in GluA1 knockout mice. Eur J Neurosci. 2017 Apr;45(7):912-

  [2]. Orlando R, et al. Levels of the Rab GDP dissociation inhibitor (GDI) are altered in the prenatal restrain stress mouse model of schizophrenia and are differentially regulated by the mGlu2/3 receptor agonists, LY379268 and LY354740. Neuropharmacology. 2014

  [3]. Procaccini C, et al. Reversal of novelty-induced hyperlocomotion and hippocampal c-Fos expression in GluA1 knockout male mice by the mGluR2/3 agonist LY354740. Neuroscience. 2013 Oct 10;250:189-200

  [4]. Lee Y, et al. The mGlu2/3 receptor agonist LY354740 suppresses immobilization stress-induced increase in rat prefrontal cortical BDNF mRNA expression. Neurosci Lett. 2006 May 8;398(3):328-32.

物理化学性质

• 密度: 1.6±0.1 g/cm3
• 沸点: 376.4±32.0 °C at 760 mmHg
• 分子式: C₈H₁₁NO₄
• 分子量: 185.18
• 闪点: 181.4±25.1 °C
• 精确质量: 185.068802
• LogP: -1.22
• InChIKey: VTAARTQTOOYTES-UHFFFAOYSA-N
• SMILES: NC1(C(=O)O)CCC2C(C(=O)O)C21
• 蒸汽压: 0.0±1.8 mmHg at 25°C
• 折射率: 1.619

靶点实验

查看更多实验

实验名称：Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells us... 来源：ChEMBL 靶标：Metabotropic glutamate receptor 3 External Id：CHEMBL713034

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：Antagonist activity against Metabotropic glutamate receptor 3 expressed in CHO cells ... 来源：ChEMBL 靶标：Metabotropic glutamate receptor 3 External Id：CHEMBL713037

实验名称：Thermal Shift Assay. Domain: start/stop: M1-L298 来源：ChEMBL 靶标：Cyclin-dependent kinase 2 External Id：CHEMBL5062802

实验名称：Inhibition of c-AMP by human Metabotropic glutamate receptor 8 (mGluR8) expressed in ... 来源：ChEMBL 靶标：Metabotropic glutamate receptor 8 External Id：CHEMBL712468

实验名称：The effective concentration for 50% glutamate response was measured on Group I Metabo... 来源：ChEMBL 靶标：N/A External Id：CHEMBL680006

实验名称：Agonist activity at human recombinant mGlu2 receptor expressed in AV12 cells assessed... 来源：ChEMBL 靶标：Metabotropic glutamate receptor 2 External Id：CHEMBL3619271

实验名称：Thermal Shift Assay. Domain: start/stop: M626-G740 来源：ChEMBL 靶标：Peregrin External Id：CHEMBL5062535

实验名称：Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 c... 来源：ChEMBL 靶标：Metabotropic glutamate receptor 3 External Id：CHEMBL3619270

实验名称：Displacement of [3H]-459477 from human recombinant mGlu2 receptor expressed in AV12 c... 来源：ChEMBL 靶标：Metabotropic glutamate receptor 2 External Id：CHEMBL3619269

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英文别名

• 8244
• LY354740
• MFCD04113018
• UNII-ONU5A67T2S
• ONU5A67T2S
• (+)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid
• l-nebivolol
• Eglumegad
• Eglumetad
• (1S,2S,5R,6S)-2-Amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
• (1S,2S,5R,6S)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid