VU 0285683

Discontinued Product

VU 0285683 (Cat. No. 4381) has been withdrawn from sale for commercial reasons.
Description: Negative allosteric modulator of mGlu5 receptors
Chemical Name: 3-Fluoro-5-[3-(2-pyridinyl)-1,2,4-oxadiazol-5-yl]-benzonitrile
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (5)

Biological Activity for VU 0285683

VU 0285683 is a 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).

Technical Data for VU 0285683

M. Wt 266.23
Formula C14H7FN4O
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 327056-22-4
PubChem ID 9816778
InChI Key GELAFISMURFRCA-UHFFFAOYSA-N
Smiles FC1=CC(C#N)=CC(C2=NC(C3=NC=CC=C3)=NO2)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

References for VU 0285683

References are publications that support the biological activity of the product.

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, VU 0285683 supplier, Negative, allosteric, modulators, mGlu5, mGluR5, mGlur, Group, I, Receptors, Glutamate, Metabotropic, MPEP, binding, site, VU0285683, nams, (Metabotropic), 4381, Tocris Bioscience

Citations for VU 0285683

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Currently there are no citations for VU 0285683.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Metabotropic Glutamate Receptors Scientific Review

Metabotropic Glutamate Receptors Scientific Review

Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.

Addiction Poster

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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.

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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.

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Huntington's disease (HD) is a severe monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the effects of mutant huntingtin aggregation implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.

Parkinson's Disease Poster

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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.