Cat. No. 2921
Chemical Name: 3-((2-Methyl-1,3-thiazol-4-yl)ethyn
Biological ActivityPotent, selective and non-competitive mGlu5 antagonist (IC50 = 5 nM in Ca2+-flux assay; Ki= 16 nM). Displays anxiolytic activity in vivo and is orally active.
Licensing InformationManufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Bradbury et al (2005) Metabotropic glutamate receptor mGlu5 is a mediator of appetite and energy balance in rats and mice. J.Pharmacol.Exp.Ther. 313 395. PMID: 15590770.
Klodzinska et al (2004) Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABAA signaling. Neuropharmacology 47 342. PMID: 15275823.
Roppe et al (2004) 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. Bioorg.Med.Chem.Lett. 14 3993. PMID: 15225713.
Cosford et al (2003) 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]- pyridine: A potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. J.Med.Chem. 46 204. PMID: 12519057.
Brodkin et al (2002) Reduced stress-induced hyperthermia in mGluR5 knockout mice. Eur.J.Neurosci. 16 2241. PMID: 12473093.
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Citations are publications that use Tocris products. Selected citations for MTEP hydrochloride include:
Arsenault et al (2015) Loss of Metabotropic Glutamate Receptor 5 Function on Peripheral Benzodiazepine Receptor in Mice Prenatally Exposed to LPS. PLoS One 10 e0142093. PMID: 26536027.
Guimaraes et al (2015) The metabotropic glutamate receptor 5 role on motor behavior involves specific neural substrates. Cell Death Dis 8 24. PMID: 25885370.
Reissner et al (2015) Glutamate transporter GLT-1 mediates N-acetylcysteine inhibition of cocaine reinstatement. Elife 20 316. PMID: 24612076.
Rosa et al (2015) Neuron-glia signaling in developing retina mediated by neurotransmitter spillover. Mol Brain 4. PMID: 26274565.
Pollard et al (2014) Modulation of neuronal microcircuit activities within the medial prefrontal cortex by mGluR5 positive allosteric modulator. J Psychopharmacol 28 935. PMID: 25031220.
Jurgens et al (2012) Optogenetic stimulation of the corticothalamic pathway affects relay cells and GABAergic neurons differently in the mouse visual thalamus. PLoS One 7 e45717. PMID: 23029198.
Sumislawski et al (2011) Reversible gating of endocannabinoid plasticity in the amygdala by chronic stress: a potential role for monoacylglycerol lipase inhibition in the prevention of stress-induced behavioral adaptation. Neuropsychopharmacology 36 2750. PMID: 21849983.
Tronson et al (2010) Metabotropic glutamate receptor 5/Homer interactions underlie stress effects on fear. Addict Biol 68 1007. PMID: 21075228.
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Keywords: MTEP hydrochloride, supplier, Potent, selective, mGlu5, mGluR5, antagonists, mGlur, Group, I, Receptors, Glutamate, Metabotropic, merck, Tocris Bioscience, Glutamate (Metabotropic) Group I Receptor Antagonist products
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