Formulation: A solid
Formal Name: 3-fluoro-5-[2-(6-methyl-2-pyridinyl)ethynyl]-benzonitrile
Purity: ≥98%
Formula Markup: C15H9FN2
Formula Weight: 236,2
Shelf life (days): 1460
CAS Number: 1224431-15-5
Notes: MFZ 10-7 is a negative allosteric modulator (NAM) and inverse agonist of metabotropic glutamate receptor 5 (mGluR5).{23785} It selectively binds to mGluR5 (Ki = 0.67 nM) over a panel of 63 additional receptors and ion channels at 100 nM. MFZ 10-7 reduces D-myo-inositol 1 phosphate (1-IP1; Item No. 1000777) accumulation, a marker of D-myo-inositol-1,4,5-triphosphate (1,4,5-IP3; Item No. 10008205) production, in an ELISA-based immunocompetitive assay using HEK293A cells expressing rat mGluR5 (IC50 = 2.4 nM). In vivo, MFZ 10-7 (0.3 mg/kg) increases the number of transitions between the light and dark area in a light-dark exploration test, indicating anxiolytic-like activity, and increases locomotor activity in the open field test in mice. It inhibits cocaine self-administration in rats when administered at doses of 3 or 10 mg/kg.{67923}
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