Cat. No. 4381
Chemical Name: 3-Fluoro-5-[3-(2-pyridinyl)-1,2,4-o
Biological ActivityNegative 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).
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All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
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 (6) 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, Tocris Bioscience, Glutamate (Metabotropic) Group I Receptor Modulator products