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).

Cell permeable: yes

Primary Target
mGluR5

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 5 nM in Ca2+-flux assay

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

Packaged under inert gas

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

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.

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

Toxicity: Standard Handling (A)