[CAS NO. 353231-17-1] LY487379
PRODUCTS SPECIFICATIONS [353231-17-1]
DESCRIPTION [353231-17-1]
Overview
| MDL | MFCD09475609 |
|---|---|
| Molecular Weight | 452.45 |
| Molecular Formula | C21H19F3N2O4S |
| SMILES | FC(F)(F)CS(=O)(N(C1=CC=C(OC2=CC=CC=C2OC)C=C1)CC3=CC=CN=C3)=O |
Summary
LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [ 35 S]GTPγS binding with EC 50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research [2] .
In Vivo
LY487379 (intraperitoneal injection; 30 mg/kg; injected 30 min before the test) requires significantly fewer trials to criterion during the ED phase of the ASST in attentional set-shifting task in male Sprague-Dawley rats. But there has no significant drug effect during any other discrimination stage
[1]
.
LY487379 hydrochloride (intraperitoneal injection; 10-30 mg/kg) induces an increase in microdialysate norepinephrine levels; the dose-effect resembled a bell-shape relationship increased. And it dose-dependently increases extracellular serotonin levels in the medial prefrontal cortex in male Sprague-Dawley rats
[1]
.
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 |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 221.02 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2102 mL | 11.0509 mL | 22.1019 mL |
| 5 mM | 0.4420 mL | 2.2102 mL | 4.4204 mL |
| 10 mM | 0.2210 mL | 1.1051 mL | 2.2102 mL |
-
1.
References
- [1] Nikiforuk A, et al. Effects of a positive allosteric modulator of group II metabotropic glutamate receptors, LY487379, on cognitive flexibility and impulsive-like responding in rats. J Pharmacol Exp Ther. 2010;335(3):665-673.
- [2] Schaffhauser H, et al. Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2. Mol Pharmacol. 2003;64(4):798-810.
Synonyms
