Negative allosteric modulator of mGlu5 receptors. Displays high affinity for the MPEP (Cat. No. 1212) binding site; acts as a full antagonist and blocks the glutamate response to mGlu5 (IC50 = 24.4 nM). Selective for mGlu5 over mGlu1, mGlu3 and mGlu4. Exhibits anxiolytic activity in rodent models of anxiety. Analog available (Cat. No. 4323).
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 266.23. 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||3.76 mL||18.78 mL||37.56 mL|
|5 mM||0.75 mL||3.76 mL||7.51 mL|
|10 mM||0.38 mL||1.88 mL||3.76 mL|
|50 mM||0.08 mL||0.38 mL||0.75 mL|
References are publications that support the products' biological activity.
Rodriguez (2010) Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity. Mol.Pharmacol. 78 1105 PMID: 20923853
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Keywords: VU 0285683, supplier, Negative, allosteric, modulators, mGlu5, mGluR5, mGlur, Group, I, Receptors, Glutamate, Metabotropic, MPEP, binding, site, VU0285683, nams, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
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