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Eglumegad is a highly effective and selective agonist of group II (mGlu2/3) receptor (IC50s: 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively).
Description | Eglumegad is a highly effective and selective agonist of group II (mGlu2/3) receptor (IC50s: 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively). |
Targets&IC50 | mGluR2R:5 nM (IC50), mGluR3R:24 nM (IC50) |
In vitro | In mouse cortical neurons, Eglumegad down-regulates spots 1014, 1822 (hypoxia up-regulated protein 1), 4513 (an isoform of protein disulfide isomerase 3), 6204, 6312, 7306 (26S proteasome non-ATPase regulatory subunit 7) and protein spots 1013 and 6005 (destrin). It also up-regulates spot 6507 (collapsin response mediator protein 1)[2]. |
In vivo | Eglumegad (15 or 30 mg/kg, i.p.) has no effect on spatial working memory performance in Gria1?/? or WT mice, and it has no effect on rewarded alternation testing with a short inter-trial interval in Gria1?/? and WT mice at a concentration of 30 mg/kg and it decreases spontaneous locomotor activity in wild-type and Gria1?/? mice[1]. Eglumegad (15 mg/kg, i.p.) reduces novelty-induced hyperlocomotion in naive GluA1-KO and pre-handled GluA1-KO males, but not in females and it also significantly reduces the increased c-Fos expression of GluA1-KO males to the level of WT males, but not in females[3]. Eglumegad (10 mg/kg, i.p.) attenuates the immobilization stress-induced increase in BDNF mRNA expression in the rat mPFC[4]. |
Alias | LY354740, Eglumetad |
Molecular Weight | 185.18 |
Formula | C8H11NO4 |
Cas No. | 176199-48-7 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | H2O: 6.33 mg/mL (34.18 mM), Sonication and heating are recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
H2O
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