MFZ 10-7 - CAS 1224431-15-5
Category: Inhibitor
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Molecular Formula:
C15H9FN2.HCl
Molecular Weight:
272.7
COA:
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Targets:
mGluR
Description:
MFZ 10-7 is a mGlu5 receptor negative allosteric modulator. It can inhibit mGlu5 glutamate-mediated calcium mobilization with IC50 value of 1.22 nM. MFZ 10-7 can inhibit cocaine-taking and cocaine-seeking behavior in rats.
Purity:
≥99% by HPLC
Synonyms:
3-Fluoro-5-[2-(6-methyl-2-pyridinyl)ethynyl]benzonitrile hydrochloride
MSDS:
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InChIKey:
ZGEXQIMQZVRTDZ-UHFFFAOYSA-N
InChI:
InChI=1S/C15H9FN2/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
Canonical SMILES:
CC1=CC=CC(=N1)C#CC2=CC(=CC(=C2)F)C#N
1.A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine-taking and cocaine-seeking behavior in rats.
Keck TM;Zou MF;Bi GH;Zhang HY;Wang XF;Yang HJ;Srivastava R;Gardner EL;Xi ZX;Newman AH Addict Biol. 2014 Mar;19(2):195-209. doi: 10.1111/adb.12086. Epub 2013 Sep 4.
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.
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CAS 1224431-15-5 MFZ 10-7

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