Biochem/physiol Actions

Cell permeable: no

Reversible: yes

Product does not compete with ATP.

Primary TargetMetabotropic glutamate receptor subtype 5 (mGluR5)

EC50 = 10 nM in potentiating the response to glutamate (~300 nM) in CHO-mGluR5 cells for human, 4-fold potentiation; 20 nM for rat, 4.3-fold potentiation

General description

A pyrazole amide compound that crosses the blood-brain barrier and acts as a potent, selective, reversible, positive allosteric modulator for metabotropic glutamate receptor subtype 5 (mGluR5). Also exerts anti-psychotic-like effects. Reported to potentiate the response to glutamate (~300 nM) in CHO-mGluR5 cells (EC₅₀ = 10 nM for human, 4-fold potentiation; 20 nM for rat, 4.3-fold potentiation) and reverse amphetamine-induced disruption of pre-pulse inhibition (PPI) in rats. Specificity was determined using a panel of kinases and receptors. Does not potentiate the activity of other glutamate receptors.

Legal Information

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

Other Notes

Kinney, G.G., et al. 2005. J. Pharmacol. Exp. Ther.313, 199.Lindsley, C.W., et al. 2004. J. Med. Chem.47, 5825.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

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)