agonist of group II mGlu receptor
CAS：176199-48-7
分子式：C8H11NO4
分子量：185.18
纯度：98%
存储：Store at -20°C
Background:
Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
Eglumegad (LY354740) 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), and up-regulates spot 6507 (collapsin response mediator protein 1) in mouse cortical neurons[2]
Eglumegad (LY354740) (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 concentration of 30 mg/kg. Eglumegad (LY354740) (15 or 30 mg/kg, i.p.) reduces spontaneous locomotor activity in wild-type and Gria1?/? mice[1]. Eglumegad (LY354740) (15 mg/kg, i.p.) dreases novelty-induced hyperlocomotion in naive GluA1-KO and pre-handled GluA1-KO males, but not in females. Eglumegad (LY354740) (15 mg/kg, i.p.) significantly reduces the increased c-Fos expression of GluA1-KO males to the level of WT males, but not in of females[3]. Eglumegad (LY354740) (10 mg/kg, i.p.) attenuates the immobilization stress-induced increase in BDNF mRNA expression in the rat mPFC[4].
Reference:
[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.
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