Description |
LY341495 is a metabotropic glutamate receptor (mGluR) antagonist with IC50s of 2.9 nM, 10 nM, 170 nM for mGluR-2, mGluR-3, mGluR-8, respectively.
|
Related Catalog |
|
Target |
IC50: 2.9 nM (mGluR-2, human), 10 nM (mGluR-3, human), 170 nM (mGluR-8, human)
|
In Vivo |
LY341495 (0.3, 1, and 3 mg/kg, i.p.) displays a lower level of discrimination in rats[1]. LY341495 (3.0 mg/kg) decreases Dvl-2, pGSK-3α/β and β-catenin protein levels but Dvl-1, Dvl-3 and GSK-3α/β are unaffected in both the PFC and STR. LY341495 has the generally the opposite effect following acute and chronic administration compared to mGlu2/3 agonist, LY379268[2]. LY341495 (3 mg/kg, i.p., 2.5 h) -induced c-Fos expression is not altered in either KO brain. LY341495 is almost inactive in the central extended amygdala [central nucleus of the amygdala, lateral (CeL) and bed nucleus of the stria terminalis, laterodorsal (BSTLD)] in mGluR3-KO mice[3].
|
Animal Admin |
The rats are randomLy divided into six experimental groups (10 rats per group): vehicle and 0.05, 0.1, 0.3, 1, and 3 mg/kg LY341495. The LY341495 doses are selected on the basis of results from previous Published studies that evaluated the effects of this compound on cognition. The rats are subjected to a training session that consisted of two 2-min trials. The animals receive either vehicle or LY341495 immediately after T1. Using the 2-min trial duration, an ITI of 1 h is used because recognition memory is still intact in untreated control rats under these experimental conditions
|
References |
[1]. Pitsikas N, et al. The metabotropic glutamate 2/3 receptor antagonist LY341495 differentially affects recognition memory in rats. Behav Brain Res. 2012 May 1;230(2):374-9. [2]. Sutton LP, et al. Regulation of Akt and Wnt signaling by the group II metabotropic glutamate receptor antagonist LY341495 and agonist LY379268.J Neurochem. 2011 Jun;117(6):973-83. [3]. Linden AM, et al. Use of MGLUR2 and MGLUR3 knockout mice to explore in vivo receptor specificity of the MGLUR2/3 selective antagonist LY341495. Neuropharmacology. 2009 Aug;57(2):172-82. Epub 2009 May 27. [4]. Li J, et al. N-acetyl-cysteine attenuates neuropathic pain by suppressing matrix metalloproteinases. Pain. 2016 Aug;157(8):1711-23.
|