Biochem/physiol Actions

Reversible: no

Primary TargetmGluR5

Target K_i: 16 nM for mGluR5 (metabotropic glutamate receptor subtype-5)

Target IC₅₀: 5 nM in Ca2+-flux assay

Product does not compete with ATP.

Cell permeable: yes

General description

A brain-permeable (thiazole-pyridine)alkyne compound that acts as a potent, selective and non-competitive mGluR5 (metabotropic glutamate receptor subtype-5) antagonist (IC₅₀ = 5 nM in Ca²⁺-flux assay; K_i = 16 nM) with in vivo anxiolytic activity in a rodent model (ED₅₀ = 1 mg/kg, ip and 7 mg/kg, po). Devoid of any side effects seen with MPEP and benzodiazepines. Reported to weakly affect the activities of other enzymes and receptors tested (IC₅₀ = 30 µM for MAO-A, >100 µM for mGlu1R, 2R & 7R, and >300 µM for NR2BR).

Legal Information

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

Other Notes

Bradbury, M.J., et al. 2005. J. Pharmacol. Exp. Ther.313, 395.Busse, C.S., et al. 2004. Neuropsychopharmacology29, 1971.Roppe, J.R., et al. 2004. Bioorg. Med. Chem. Lett.14, 3993.Klodzinska, A., et al. 2004. Neuropharmacology47, 342.Cosford, N.D.P., et al. 2003. J. Med. Chem.46, 204.Brodkin, J., et al. 2002. Eur. J. Neurosci.16, 2241.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

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)