Details
Stereochemistry | ACHIRAL |
Molecular Formula | C15H9FN2 |
Molecular Weight | 236.2438 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=NC(=CC=C1)C#CC2=CC(=CC(F)=C2)C#N
InChI
InChIKey=ZGEXQIMQZVRTDZ-UHFFFAOYSA-N
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
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/21546249
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21546249
MFZ 10-7 is a high affinity negative allosteric modulator at the mGlu5 receptor (Ki = 0.67 nM). MFZ 10-7 demonstrates anxyolitic properties in mouse models. 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.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P41594 Gene ID: 2915.0 Gene Symbol: GRM5 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/21546249 |
1.22 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series. | 2011 Jun 1 |
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Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. | 2012 Jul 12 |
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A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine-taking and cocaine-seeking behavior in rats. | 2014 Mar |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22924094
For anxyolitic tests MFZ 10-7 was delivered via ip injection 15 min prior to testing. Anxyolitic effects were observed at dose 0.3 mg/kg.
Route of Administration:
Intraperitoneal
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21546249
MFZ 10-7 was evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro assay. MFZ 10-7 (compound 2d) inhibited mGluR5 with IC50 1.22 nM.
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1224431-15-5
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FV36HKQ9RA
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46208250
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MFZ 10-7
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DTXSID501336029
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SALT/SOLVATE (PARENT)
SALT/SOLVATE (PARENT)
SUBSTANCE RECORD