MTEP

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Chemical compound

title: "MTEP" type: doc version: 1 created: 2026-02-28 author: "Wikipedia contributors" status: active scope: public tags: ["thiazoles", "3-pyridyl-compounds", "alkyne-derivatives", "mglu5-receptor-antagonists"] description: "Chemical compound" topic_path: "general/thiazoles" source: "https://en.wikipedia.org/wiki/MTEP" license: "CC BY-SA 4.0" wikipedia_page_id: 0 wikipedia_revision_id: 0

::summary Chemical compound ::

::callout[type=note] MTEP also stands for Magnetothermoelectric Power, for the Medium Term Economic Program, for the Medium-Term Employment Plan, for the OECD's Medium-Term Expenditure Programme, for the [[MISO Transmission Expansion Plan ::

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| tradename = | pregnancy_AU = | pregnancy_US = | legal_AU = | legal_CA = | legal_UK = | legal_US =

| IUPHAR_ligand = 3336 | CAS_number_Ref = | CAS_number = 329205-68-7 | UNII_Ref = | UNII = XDA7P9K5S6 | PubChem = 9794218 | ChemSpiderID_Ref = | ChemSpiderID = 7969985

| C=11 | H=8 | N=2 | S=1 | smiles = CC1=NC(=CS1)C#CC2=CN=CC=C2 | StdInChI_Ref = | StdInChI = 1S/C11H8N2S/c1-9-13-11(8-14-9)5-4-10-3-2-6-12-7-10/h2-3,6-8H,1H3 | StdInChIKey_Ref = | StdInChIKey = NRBNGHCYDWUVLC-UHFFFAOYSA-N

3-((2-Methyl-4-thiazolyl)ethynyl)pyridine (MTEP) is a research drug that was developed by Merck & Co. as a selective allosteric antagonist of the metabotropic glutamate receptor subtype mGluR5. Identified through structure-activity relationship studies on an older mGluR5 antagonist MPEP, MTEP has subsequently itself acted as a lead compound for newer and even more improved drugs.

MTEP is both more potent and more selective than MPEP as a mGluR5 antagonist, and produces similar neuroprotective, antidepressant, analgesic, and anxiolytic effects but with either similar or higher efficacy depending on the test used.

MTEP also has similar efficacy to MPEP in reducing the symptoms of morphine withdrawal, and has anti-addictive effects in a variety of animal models, both reducing ethanol self-administration, and also decreasing the addictive effects of nicotine, cocaine and methamphetamine.

References

References

  1. (January 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". Journal of Medicinal Chemistry.
  2. (February 2006). "Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications". Journal of Medicinal Chemistry.
  3. (June 2007). "Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists". Bioorganic & Medicinal Chemistry Letters.
  4. (2006). "Metabotropic glutamate receptor subtype 5 antagonists MPEP and MTEP". CNS Drug Reviews.
  5. (June 2005). "Neuroprotective activity of the mGluR5 antagonists MPEP and MTEP against acute excitotoxicity differs and does not reflect actions at mGluR5 receptors". British Journal of Pharmacology.
  6. (2006). "Neuroprotective effects of MTEP, a selective mGluR5 antagonists and neuropeptide Y on the kainate-induced toxicity in primary neuronal cultures". Pharmacological Reports.
  7. (January 2007). "Neuroprotective activity of selective mGlu1 and mGlu5 antagonists in vitro and in vivo". European Journal of Pharmacology.
  8. (August 2005). "Potential antidepressant-like effect of MTEP, a potent and highly selective mGluR5 antagonist". Pharmacology, Biochemistry, and Behavior.
  9. (August 2006). "Antidepressant-like and anxiolytic-like actions of the mGlu5 receptor antagonist MTEP, microinjected into lateral septal nuclei of male Wistar rats". Progress in Neuro-Psychopharmacology & Biological Psychiatry.
  10. (October 2006). "Metabotropic glutamate 5 receptor antagonism is associated with antidepressant-like effects in mice". The Journal of Pharmacology and Experimental Therapeutics.
  11. (February 2007). "Antidepressant-like effects of mGluR1 and mGluR5 antagonists in the rat forced swim and the mouse tail suspension tests". European Neuropsychopharmacology.
  12. (December 2004). "Assessing the role of metabotropic glutamate receptor 5 in multiple nociceptive modalities". European Journal of Pharmacology.
  13. (April 2005). "The antinociceptive and anxiolytic-like effects of the metabotropic glutamate receptor 5 (mGluR5) antagonists, MPEP and MTEP, and the mGluR1 antagonist, LY456236, in rodents: a comparison of efficacy and side-effect profiles". Psychopharmacology.
  14. (September 2004). "Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABA(A) signaling". Neuropharmacology.
  15. (November 2004). "The behavioral profile of the potent and selective mGlu5 receptor antagonist 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) in rodent models of anxiety". Neuropsychopharmacology.
  16. (May 2005). "Anxiolytic-like effects of mGlu1 and mGlu5 receptor antagonists in rats". European Journal of Pharmacology.
  17. (November 2007). "Anxiolytic-like action of MTEP expressed in the conflict drinking Vogel test in rats is serotonin dependent". Neuropharmacology.
  18. (2004). "Selective mGlu5 receptor antagonist MTEP attenuates naloxone-induced morphine withdrawal symptoms". Polish Journal of Pharmacology.
  19. (February 2005). "The mGlu5 receptor antagonists MPEP and MTEP attenuate behavioral signs of morphine withdrawal and morphine-withdrawal-induced activation of locus coeruleus neurons in rats". Neuropharmacology.
  20. (March 2007). "Comparison of the effects of mGluR1 and mGluR5 antagonists on the expression of behavioral sensitization to the locomotor effect of morphine and the morphine withdrawal jumping in mice". European Journal of Pharmacology.
  21. (November 2005). "The metabotropic glutamate 5 receptor antagonist 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-pyridine reduces ethanol self-administration in multiple strains of alcohol-preferring rats and regulates olfactory glutamatergic systems". The Journal of Pharmacology and Experimental Therapeutics.
  22. (January 2007). "Assessing appetitive and consummatory phases of ethanol self-administration in C57BL/6J mice under operant conditions: regulation by mGlu5 receptor antagonism". Psychopharmacology.
  23. (March 2008). "Combined antagonism of glutamate mGlu5 and adenosine A2A receptors interact to regulate alcohol-seeking in rats". The International Journal of Neuropsychopharmacology.
  24. (November 2008). "The influence of various glutamate receptors antagonists on anxiety-like effect of ethanol withdrawal in a plus-maze test in rats". European Journal of Pharmacology.
  25. (September 2006). "Effects of group I metabotropic glutamate receptor antagonists on the behavioral sensitization to motor effects of cocaine in rats". Psychopharmacology.
  26. (August 2008). "Metabotropic glutamate 5 receptor (mGluR5) antagonists decrease nicotine seeking, but do not affect the reinforcement enhancing effects of nicotine". Neuropsychopharmacology.
  27. (March 2009). "mGluR5 antagonism attenuates methamphetamine reinforcement and prevents reinstatement of methamphetamine-seeking behavior in rats". Neuropsychopharmacology.
  28. (October 2008). "A role for mGluR5 receptors in intravenous methamphetamine self-administration". Annals of the New York Academy of Sciences.
  29. (June 2009). "Dissociation of the effects of MTEP [3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]piperidine] on conditioned reinstatement and reinforcement: comparison between cocaine and a conventional reinforcer". The Journal of Pharmacology and Experimental Therapeutics.

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thiazoles3-pyridyl-compoundsalkyne-derivativesmglu5-receptor-antagonists