Eglumegad

Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC₅₀s of 5 nM and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively. In Vitro: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]. In Vivo: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].