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LY404039 is a potent, selective and orally active agonist for the metabotropic glutamate receptor (mGluR)2/3 receptors. mGluR2 acts as a glutamatergic autoreceptor in the brain regions that are believed to be important in the pathophysiology of schizophrenia, such as the prefrontal cortex, striatum, hippocampal formation and the thalamus. LY404039 potently inhibits forskolin-stimulated cAMP formation in cells expressing human mGlu2 and mGlu3 receptors. LY404039 reduces responding on the EtOH in the pavlovian spontaneous recovery (PSR) test and reduces the expression of an alcohol deprivation effect (ADE) during relapse, but does not affect EtOH responding under maintenance conditions. LY404039 also increases dopamine and serotonin release/turnover in the prefrontal cortex.
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Source | Pharmacol Res Perspect (2015). Figure 2. LY404039 |
| Method | s.c. | |
| Cell Lines | Mice | |
| Concentrations | 0.63, 2.5, 10 mg/kg | |
| Incubation Time | 0.5 h | |
| Results | JNJ-40411813, JNJ-42153605, and LY404039 dose dependently inhibited spontaneous locomotion and PCP- and scopolamine-induced hyperlocomotion but not damphetamine- induced hyperlocomotion |
| Cell Experiment | |
|---|---|
| Cell lines | RGT cells expressing human mGlu receptors |
| Preparation method | For cAMP assays, cells expressing human mGlu2, mGlu3, mGlu4, mGlu6, mGlu7, or mGlu8 were washed (two times with 200 μl/well) with assay medium (Dulbecco's phosphate-buffered saline plus 3 mM glucose and 500 μM isobutymethylxanthine). The media were replaced with 0.2 ml/well of the same solution, and cells were preincubated for 30 min at 37°C under 95% O2, 5%CO2. Each well was then washed two successive times with 200 μl of medium. Compounds of interest or water vehicle were added, along with forskolin solution (15 μM final concentration group II mGlu receptors, 1 μM final concentration group III mGlu receptors, and total incubation volume 0.1 ml), and cells were further incubated at 37°C under 95% O2, 5%CO2 for 20 min. The incubation was terminated by adding 0.1 ml of 0.2% Triton X-100 lysing solution. Levels of cAMP were determined by a cAMP-125I Scintillation Proximity Assay Screening Biotrak Assay kit (GE Healthcare). |
| Concentrations | 0~10mM |
| Incubation time | 20 min |
| Animal Experiment | |
|---|---|
| Animal models | PCP-Induced mouse model |
| Formulation | 0.9% saline |
| Dosages | 10 mg/kg |
| Administration | i.p. |
| Molecular Weight | 235.21 |
| Formula | C7H9NO6S |
| CAS Number | 635318-11-5 |
| Solubility (25°C) | DMSO 1 mg/mL (Need ultrasonic) Water 1 mg/mL (ultrasonic and adjust pH to 6 with NaOH) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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