Biological Activity
Potent and selective positive allosteric modulator at the mGlu5 receptor (EC50 = 24 nM). Has no activity at mGlu1-4, mGlu8 and GABAB receptors. Reverses methylazoxymethanol acetate (MAM)-induced deficits in reversal learning memory and normalizes SDZ 220-581 and RO 63-1908-induced alterations in instrumental responses in rat models. Promotes wakefulness in vivo. Brain penetrant and orally active.
Compound Libraries
LSN 2463359 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 265.31 |
| Formula | C16H15N3O |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1401031-52-4 |
| PubChem ID | 72551298 |
| InChI Key | STAFRSGTRKNXHF-UHFFFAOYSA-N |
| Smiles | O=C(NC(C)C)C(C=C2)=NC=C2C#CC1=CC=NC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 26.53 | 100 | |
| ethanol | 5.31 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 265.31. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.77 mL | 18.85 mL | 37.69 mL |
| 5 mM | 0.75 mL | 3.77 mL | 7.54 mL |
| 10 mM | 0.38 mL | 1.88 mL | 3.77 mL |
| 50 mM | 0.08 mL | 0.38 mL | 0.75 mL |
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References
References are publications that support the products' biological activity.
Gastambide et al (2012) Selective remediation of reversal learning deficits in the neurodevelopmental MAM model of schizophrenia by a novel mGlu5 positive allosteric modulator. Neuropsychopharmacology 37 1057 PMID: 22129780
Gilmour et al (2013) In vitro characterisation of the novel positive allosteric modulators of the mGlu5 receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat. Neuropharmacology 64 224 PMID: 22884720
Gastambide et al (2013) The mGlu5 positive allosteric modulator LSN2463359 differentially modulates motor, instrumental and cognitive effects of NMDA receptor antagonists in the rat. Neuropharmacology 64 240 PMID: 22884612
Keywords: LSN 2463359, supplier, LSN2463359, potent, selective, positive, allosteric, modulator, PAM, MGLU5, brain, penetrant, orally, active, schizophrenia, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
