Potent, 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.
Manufactured 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)
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 236.72. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||4.22 mL||21.12 mL||42.24 mL|
|5 mM||0.84 mL||4.22 mL||8.45 mL|
|10 mM||0.42 mL||2.11 mL||4.22 mL|
|50 mM||0.08 mL||0.42 mL||0.84 mL|
References are publications that support the products' biological activity.
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
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
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
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
If you know of a relevant reference for MTEP hydrochloride, please let us know.
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Keywords: MTEP hydrochloride, supplier, Potent, selective, mGlu5, mGluR5, antagonists, mGlur, Group, I, Receptors, Glutamate, Metabotropic, merck, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
8 Citations for MTEP hydrochloride
Citations are publications that use Tocris products. Selected citations for MTEP hydrochloride include:
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
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
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
Guimaraes et al (2015) The metabotropic glutamate receptor 5 role on motor behavior involves specific neural substrates. Cell Death Dis 8 24 PMID: 25885370
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
Tronson et al (2010) Metabotropic glutamate receptor 5/Homer interactions underlie stress effects on fear. Addict Biol 68 1007 PMID: 21075228
Do you know of a great paper that uses MTEP hydrochloride from Tocris? If so please let us know.
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