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mGluR5 Antagonist, MTEP - CAS 329205-68-7 - Calbiochem

The mGluR5 Antagonist, MTEP, also referenced under CAS 329205-68-7, controls the biological activity of mGluR5. This small molecule/inhibitor is primarily used for Neuroscience applications.

Synonym: 3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine, mGluR5 Antagonist, MTEP - CAS 329205-68-7 - Calbiochem

  • CAS Number 329205-68-7

  • Empirical Formula (Hill Notation) C11H8N2S

  • Molecular Weight 200.26

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Properties

Related Categories Cell Biology, Cell Signaling and Neuroscience, Extracellular Matrix Peptides (ECM), Ion Channels, Ionotropic Glutamate Receptor Modulators,
Quality Level   100
assay   ≥98% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   white to yellow
solubility   methanol: 1 mg/mL
  DMSO: 5 mg/mL
shipped in   ambient

Description

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; Ki = 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).

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; Ki = 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).

Packaging

5 mg in Plastic ampoule

Biochem/physiol Actions

Cell permeable: yes

Primary Target
mGluR5

Product does not compete with ATP.

Reversible: no

Target IC50: 5 nM in Ca2+-flux assay

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

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.

Safety & Documentation

Safety Information

Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable
Protocols & Articles
Peer-Reviewed Papers
15

References

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