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Submit ReviewVU 0424465
Discontinued Product
6895 has been discontinued.
View all Glutamate (Metabotropic) Group I Receptors products.
Description: Potent mGlu5 positive allosteric modulator and agonist; binds allosteric site with high affinity
Chemical Name: 5-[2-(2-(3-Fluorophenyl)ethynyl]-N-[(1R)-2-hydroxy-1,2-dimethylpropyl]-2-pyridinecarboxamide
Purity: ≥98% (HPLC)
Biological Activity for VU 0424465
VU 0424465 is a potent mGlu5 positive allosteric modulator (EC50 = 1.5 nM) and agonist (EC50 = 171 nM; maximum effect is 65% that of glutamate). Binds allosteric site with high affinity (Ki = 11.8 nM). Increases maximum response to glutamate by 30%. Exhibits bias towards signaling via IP1 and ERK1/2 over iCa2+ in HEK293 and neuronal cells, and activates Gs in HEK 293 cells. Induces epileptiform activity in CA3 hippocampal neurons in vitro and convulsions in vivo.
Technical Data for VU 0424465
| M. Wt | 326.37 |
| Formula | C19H19FN2O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1428630-85-6 |
| PubChem ID | 53384864 |
| InChI Key | ZPKZAFDYFVJULO-CYBMUJFWSA-N |
| Smiles | C[C@H](C(C)(O)C)NC(C1=CC=C(C#CC2=CC(F)=CC=C2)C=N1)=O |
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.
Product Datasheets for VU 0424465
References for VU 0424465
References are publications that support the biological activity of the product.
Rook et al (2013) Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity. Biol.Psychiatry. 73 501 PMID: 23140665
Sengmany et al (2017) Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology 115 60 PMID: 27392634
Nasrallah et al (2018) Direct coupling of detergent purified human mGlu5 receptor to the heterotrimeric G proteins Gq and Gs. Sci.Rep. 8 4407 PMID: 29535347
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Keywords: VU 0424465, VU 0424465 supplier, VU0424465, metabotropic, glutamate, receptor, subtype, 5, mGlu5, mGluR, agonist, positive, allosteric, modulators, modulates, agonists, agonism, potent, high, affinity, Glutamate, (Metabotropic), Group, I, Receptors, 6895, Tocris Bioscience
Citations for VU 0424465
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Currently there are no citations for VU 0424465.
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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
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.
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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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Huntington's Disease Poster
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Parkinson's Disease Poster
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.