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Products are for research use only. Not for human use. We do not sell to patients.
(LY 341495; LY-341495)
LY341495 Chemical Structure
|Product name: LY341495|
|Cat. No.: HY-70059|
LY341495 is a highly potent and selective group II metabotropic glutamate receptor antagonist. (Ki/IC50 values are 2.3, 1.3, 173, 990, 6800, 8200 and 22000 nM for human mGlu2, mGlu3, mGlu8 , mGlu7a, mGlu1a, mGlu5a and mGlu4a receptors respectively).
IC50 Value: 2.9 nM (for mGluR-2, human); 10 nM (for mGluR-3, human); 170 nM (for mGluR-8, huma)
in vitro: LY341495 was micromolar potent in antagonizing quisqualate-induced phosphoinositide (PI) hydrolysis, with IC50 values of 7.8 and 8.2 microM for mGlu1a and mGlu5a receptors, respectively. Among the human group III mGlu receptors, the most potent inhibition of L-2-amino-4-phosphonobutyric acid (L-AP4) responses was seen for LY341495 at mGlu8, with an IC50 of 0.17 microM. LY341495 was less potent at mGlu7 (IC50 = 0.99 microM) and least potent at mGlu4 (IC50 = 22 microM). LY341495 competitively antagonised DHPG-stimulated PI hydrolysis in AV12-664 cells expressing either human mGlu1 or mGlu5 receptors with Ki-values of 7.0 and 7.6 microM, respectively.
in vivo: LY341495 (3 mg/kg, i.p., 2.5 h) -induced c-Fos expression was not altered in either KO brain. However, in mGluR3-KO mice, LY341495 was almost inactive in the central extended amygdala [central nucleus of the amygdala, lateral (CeL) and bed nucleus of the stria terminalis, laterodorsal (BSTLD)].
|M.Wt||353.37||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.8299 mL||14.1495 mL||28.2990 mL|
|5 mM||0.5660 mL||2.8299 mL||5.6598 mL|
|10 mM||0.2830 mL||1.4149 mL||2.8299 mL|
. 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.
. Bespalov AY, et al. Behavioral characterization of the mGlu group II/III receptor antagonist, LY-341495, in animal models of anxiety and depression.Eur J Pharmacol. 2008 Sep 11;592(1-3):96-102. Epub 2008 Jul 2.
. Ornstein, P.L, et al., 2-substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 2. Effects of aromatic substitution, pharmacological characterization, and bioavailability. J Med Chem, 1998. 41(3): p. 358-78.
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