MFZ 10-7Negative allosteric modulator at mGlu5 CAS# 1224431-15-5 |
2D Structure
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
Cas No. | 1224431-15-5 | SDF | Download SDF |
PubChem ID | 90488944 | Appearance | Powder |
Formula | C15H10ClFN2 | M.Wt | 272.7 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble to 100 mM in DMSO and to 100 mM in ethanol | ||
Chemical Name | 3-fluoro-5-[2-(6-methylpyridin-2-yl)ethynyl]benzonitrile;hydrochloride | ||
SMILES | CC1=CC=CC(=N1)C#CC2=CC(=CC(=C2)F)C#N.Cl | ||
Standard InChIKey | WRHOKQFFLQKKNL-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C15H9FN2.ClH/c1-11-3-2-4-15(18-11)6-5-12-7-13(10-17)9-14(16)8-12;/h2-4,7-9H,1H3;1H | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | High affinity negative allosteric modulator at the mGlu5 receptor (Ki = 0.67 nM). Potently inhibits mGlu5 glutamate-mediated calcium mobilization (IC50 = 1.22 nM). Inhibits cocaine-taking and cocaine-seeking behavior in rats. |
MFZ 10-7 Dilution Calculator
MFZ 10-7 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 3.667 mL | 18.3352 mL | 36.6703 mL | 73.3407 mL | 91.6758 mL |
5 mM | 0.7334 mL | 3.667 mL | 7.3341 mL | 14.6681 mL | 18.3352 mL |
10 mM | 0.3667 mL | 1.8335 mL | 3.667 mL | 7.3341 mL | 9.1676 mL |
50 mM | 0.0733 mL | 0.3667 mL | 0.7334 mL | 1.4668 mL | 1.8335 mL |
100 mM | 0.0367 mL | 0.1834 mL | 0.3667 mL | 0.7334 mL | 0.9168 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine-taking and cocaine-seeking behavior in rats.[Pubmed:24001208]
Addict Biol. 2014 Mar;19(2):195-209.
Pre-clinical studies suggest that negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 5 (mGluR5), including 2-methyl-6-(phenylethynyl)pyridine (MPEP), 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) and fenobam are highly effective in attenuating drug-taking and drug-seeking behaviors. However, both MPEP and MTEP have no translational potential for use in humans because of their off-target effects and short half-lives. Here, we report that 3-fluoro-5-[(6-methylpyridin-2-yl)ethynyl]benzonitrile (MFZ 10-7), a novel mGluR5 NAM, is more potent and selective than MPEP, MTEP and fenobam in both in vitro binding and functional assays. Similar to MTEP, intraperitoneal administration of MFZ 10-7 inhibited intravenous cocaine self-administration, cocaine-induced reinstatement of drug-seeking behavior and cocaine-associated cue-induced cocaine-seeking behavior in rats. Although MFZ 10-7 and MTEP lowered the rate of oral sucrose self-administration, they did not alter total sucrose intake. Further, MFZ 10-7 appeared to be more potent than MTEP in inducing downward shifts in the cocaine dose-response curve, but less effective than MTEP in attenuating sucrose-induced reinstatement of sucrose-seeking behavior. MFZ 10-7 and MTEP had no effect on basal locomotor behavior. These findings not only provide additional evidence supporting an important role for mGluR5 in cocaine reward and addiction, but also introduce a new tool for both in vitro and in vivo investigations with which to further characterize this role.
Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation.[Pubmed:22924094]
ACS Med Chem Lett. 2012 Jul 12;3(7):544-549.
Negative allosteric modulators (NAMs) of metabotropic glutamate receptor subtype 5 (mGluR5) have shown promising results in preclinical models for anxiety and drug abuse. Here we describe a series of aryl-substituted alkynyl analogues of the prototypic mGluR5 NAM 2-methyl-6-(phenylethynyl)pyridine (MPEP, 1). Displacement of [(3)H]1 binding in rat brain membranes showed that several of these novel compounds displayed high affinity binding (K(i) < 10 nM) for mGluR5, with up to a 24-fold increase in affinity over 1. Replacements of the 2-position Me on the pyridyl ring of 1 along with various 3'-CN, 5'-substitutions were generally well tolerated. All of the active analogues in this series had cLogP values in the 2-5 range and displayed inverse agonist characteristics in an ELISA-based assay of G(q)alpha-mediated IP3 production. Compounds 7i and 7j produced in vivo effects in mouse models of anxiety-like behaviors more potently than 1 or 3-((2-methyl-1,3-thiazol-4-yl)ethynyl)pyridine (MTEP, 2), supporting their utility as in vivo tools.
Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.[Pubmed:21546249]
Bioorg Med Chem Lett. 2011 Jun 1;21(11):3243-7.
We report the synthesis of four series of 3,5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5: (2-methylthiazol-4-yl)ethynyl (1a-j,), (6-methylpyridin-2-yl)ethynyl (2a-j), (5-methylpyridin-2-yl)ethynyl (3a-j,), and (pyridin-2-yl)ethynyl (4a-j,). The compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro assay. All compounds were found to be full antagonists and exhibited low nanomolar to subnanomolar activity.