|Description|| Potent, highly selective, non-competitive mGluR5 antagonist |
|Biological description|| |
MTEP hydrochloride is a potent, highly selective and non-competitive mGlu5 receptor antagonist (IC50 = 5 nM and Ki = 16 nM in an in vitro Ca2+-flux assay).
MTEP has no significant effect on other mGluRs and shows fewer off-target effects than MPEP hydrochloride. MTEP shows ~10-fold greater selectivity for mGlu5 than MPEP.
MTEP also blocks induction of tLTP (timing-dependent long term potentiation) and has antidepressant, anxiolytic and neuroprotective properties.
MTEP is active in vivo.
Solubility & Handling
|Storage instructions|| +4°C (desiccate) |
|Solubility overview|| Soluble in water (100mM) and in DMSO (100mM) |
|Important|| This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use. |
|Chemical name|| 3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine hydrochloride |
|Chemical structure|| |
|Molecular Formula|| C11H8N2S.HCl |
|PubChem identifier|| 45073467 |
|SMILES|| CC1=NC(=CS1)C#CC2=CN=CC=C2.Cl |
|InChi|| InChI=1S/C11H8N2S.ClH/c1-9-13-11(8-14-9)5-4-10-3-2-6-12-7-10;/h2-3,6-8H,1H3;1H |
|InChiKey|| YCIOJDKGCWAHLR-UHFFFAOYSA-N |
|Appearance|| Light cream solid |
References for MTEP hydrochloride
References are publications that support the biological activity of the product
Gating of NMDA receptor-mediated hippocampal spike timing-dependent potentiation by mGluR5.
Kwag and Paulsen (2012) Neuropharmacology 63(4) : 701-9
Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation.
Keck TM et al (2012) ACS Med Chem Lett 3(7) : 544-549.
NMDA but not AMPA glutamatergic receptors are involved in the antidepressant-like activity of MTEP during the forced swim test in mice.
Pomierny-Chamioło L et al (2010) Pharmacol Rep 62(6) : 1186-90.
Neuroprotective potential of mGluR5 antagonist MTEP: effects on kainate-induced excitotoxicity in the rat hippocampus.
Domin H et al (2010) Pharmacol Rep 62(6) : 1051-61.
Metabotropic glutamate receptor subtype 5 antagonists MPEP and MTEP.
Lea and Faden (2006) CNS Drug Rev. 12(2) : 149-66
These publications cite the use of MTEP hydrochloride purchased from Hello Bio:
Long-term synaptic depression triggers local biogenesis of autophagic vesicles in dendrites and requires autophagic degradation
Kallergi et al. (2020) bioRxiv preprint : 1-46
The role of glutamate mGlu5 and adenosine A2a receptor interactions in regulating working memory performance and persistent cocaine seeking in rats
Hamor et al (2020) Prog Neuropsychopharmacol Biol Psychiatry : doi: 10.1016/j.pnpbp.2020.109979
An Appraisal of the Influence of the Metabotropic Glutamate 5 (mGlu5) Receptor on Sociability and Anxiety.
Ramos-Prats et al (2019) Front Mol Neurosci. 19 : 12:30