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Biological Activity for MTEP hydrochloride
MTEP hydrochloride is a 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)
Compound Libraries for MTEP hydrochloride
Technical Data for MTEP hydrochloride
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for MTEP hydrochloride
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for MTEP hydrochloride
The following data is based on the product molecular weight 236.72. Batch specific molecular weights may vary from batch to batch due to the degree 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|
Product Datasheets for MTEP hydrochloride
References for MTEP hydrochloride
References are publications that support the biological activity of the product.
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, MTEP hydrochloride supplier, Potent, selective, mGlu5, mGluR5, antagonists, mGlur, Group, I, Receptors, Glutamate, Metabotropic, merck, (Metabotropic), 2921, Tocris Bioscience
11 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
Ren et al (2012) Intrathecal injection of metabotropic glutamate receptor subtype 3 and 5 agonist/antagonist attenuates bone cancer pain by inhibition of spinal astrocyte activation in a mouse model. Anesthesiology 116 122 PMID: 22123524
Thomson et al (2017) Cell-Type-Specific Translation Profiling Reveals a Novel Strategy for Treating Fragile X Syndrome. Neuron 95 550 PMID: 28772121
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
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
Lim et al (2018) Neuronal Activity-Dependent Activation of Astroglial Calcineurin in Mouse Primary Hippocampal Cultures. Int J Mol Sci 19 PMID: 30274399
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? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Huntington's Disease Poster
Huntington's disease (HD) is a monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the MSN intracellular signaling pathways implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.