[CAS NO. 201943-63-7] LY341495
PRODUCTS SPECIFICATIONS [201943-63-7]
DESCRIPTION [201943-63-7]
Overview
| MDL | MFCD00949707 |
|---|---|
| Molecular Weight | 353.37 |
| Molecular Formula | C20H19NO5 |
| SMILES | O=C(O)[C@@H]1[C@H](C1)[C@@](N)(CC2C3=C(C=CC=C3)OC4=C2C=CC=C4)C(O)=O |
5 Publications Citing Use of MCE
Summary
LY341495 is a metabotropic glutamate receptor (mGluR) antagonist with IC 50 s of 21 nM, 14 nM, 7.8 μM, 8.2 μM, 170 nM, 990 nM, 22 μM for mGlu2, mGlu3, mGlu1a, mGlu5a, mGlu8, mGlu7, and mGlu4 receptors, respectively [5] .
IC50 & Target
|
mGluR1a 7.8 μM (IC 50 ) |
mGluR2 21 nM (IC 50 ) |
mGluR3 14 nM (IC 50 ) |
mGluR4 22 μM (IC 50 ) |
mGluR5a 8.2 μM (IC 50 ) |
mGluR7 990 nM (IC 50 ) |
mGluR8 170 nM (IC 50 ) |
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 6 mg/mL ( 16.98 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 0.6 mg/mL (1.70 mM); Clear solution
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.
- [5] A E Kingston, et al. LY341495 Is a Nanomolar Potent and Selective Antagonist of Group II Metabotropic Glutamate Receptors.Neuropharmacology. 1998;37(1):1-12.
Synonyms
