176027-90-0

• 常用中文名：Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1R,2R,5S,6R)-rel- (9CI)
• 常用英文名：Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1R,2R,5S,6R)-rel- (9CI)
• CAS号：176027-90-0
• 分子式：C₈H₁₁NO₄
• 分子量：185.18
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 谷氨酸受体
• 发布时间：2021-09-11 13:51:09
• 更新时间：2024-04-06 17:12:25
• (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
• 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; Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1S,2S,5R,6S)-; (1S,2S,5R,6S)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid

物化性质

• 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
• 蒸汽压: 0.0±1.8 mmHg at 25°C
• 折射率: 1.619

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:

  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.