Biochem/physiol Actions

Reversible: yes

Target IC₅₀: 3.5 and 2.8 µ

Primary TargetmGlu7R

Cell permeable: yes

General description

A blood-brain barrier permeable and bioavailable chromenone compound that acts as a potent, selective, and reversible antagonist of mGlu7 receptor (IC₅₀ = 3.5 and 2.8 µM for mGlu7a and mGlu7b in CHO cells). Docks within the Venus flytrap domain (VFTD) close to the binding site of L-glutamate and functions as an orthosteric-like antagonist. Reduces DL-2-amino-4-phosphonobutyric acid (DL-AP4)-induced activation of human mGlu7b receptor (IC₅₀ = 2.8 µM), but does not affect DL-AP4-induced activation of [³⁵S]GTPγS binding by mGlu4 and mGlu6. Shown to diminish [³⁵S]GTPγS binding by the human mGlu7/6 chimeric receptor harboring mGlu7 VFTD (IC₅₀ = 2.5 µM). Displays weak binding affinity towards mGlu5 and mGlu8 receptors (IC₅₀ >20 and 33 µM, respectively) and has no effect on GABA-induced activation of [³⁵S]GTPγS binding by GABA-B receptors. Displays antidepressant and anxiolytic-like properties and selectively blocks long-term potentiation (LTP) in the lateral amygdala of wild type (IC₅₀ = 88 nM), but not of mGlu7- deficient mice.Please note that the molecular weight for this compound is batch-specific due to variable water content.

A blood-brain barrier permeable and bioavailable chromenone compound that acts as a potent, selective, and reversible antagonist of mGlu7 receptor (IC₅₀ = 3.5 and 2.8 µM for mGlu7a and mGlu7b in CHO cells). Docks within the Venus flytrap domain (VFTD) close to the binding site of L-glutamate and functions as an orthosteric-like antagonist. Reduces DL-2-amino-4-phosphonobutyric acid (DL-AP4)-induced activation of human mGlu7b receptor (IC₅₀ = 2.8 µM), but does not affect DL-AP4-induced activation of [³⁵S]GTPγS binding by mGlu4 and mGlu6. Shown to diminish [³⁵S]GTPγS binding by the human mGlu7/6 chimeric receptor harboring mGlu7 VFTD (IC₅₀ = 2.5 µM). Displays weak binding affinity towards mGlu5 and mGlu8 receptors (IC₅₀ >20 and 33 µM, respectively) and has no effect on GABA-induced activation of [³⁵S]GTPγS binding by GABA-B receptors. Displays antidepressant and anxiolytic-like properties and selectively blocks long-term potentiation (LTP) in the lateral amygdala of wild type (IC₅₀ = 88 nM), but not of mGlu7- deficient mice.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Gee, C.E., et al. 2014. J. Biol. Chem.289, 10975.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)