MTEP hydrochloride

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Cat.No. 2921 - MTEP hydrochloride | C11H8N2S.HCl | CAS No. 1186195-60-7
Description: Potent, selective mGlu5 antagonist
Chemical Name: 3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (8)
Literature

Biological Activity

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.

Licensing Information

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)

Technical Data

M. Wt 236.72
Formula C11H8N2S.HCl
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 1186195-60-7
PubChem ID 45073467
InChI Key YCIOJDKGCWAHLR-UHFFFAOYSA-N
Smiles CC1=NC(C#CC2=CN=CC=C2)=CS1.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 23.67 100
water 23.67 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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


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8 Citations for MTEP hydrochloride

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

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

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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