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Category: 7TM ReceptorsarrowGlutamate (Metabotropic) ReceptorsarrowGroup I mGlu ReceptorsarrowAntagonists
Cat.No. Product Name
2921

MTEP

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(Please read important notice below)
Chemical Name: 3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine

Biological Activity:

A potent, selective and non-competitive mGlu5 antagonist (IC50 = 5 nM in Ca2+-flux assay; Ki= 16 nM).

Important Notice:

Tocris’ policy is to never knowingly supply research products against the wishes of the patent holder, helping our customers to ensure compliance with their organisation’s purchasing policies and avoid any threat of possible legal action arising from the use of unapproved, unlicensed products1.

In the case of MTEP, Tocris has been in ongoing discussion with the patent holders Merck & Co. to ask whether they would allow MTEP to be made commercially available by us for research use. Merck’s position at this time is that they do not want MTEP available for sale as a laboratory research reagent, because it remains of potential development interest to them.

Despite this, regrettably a number of other life science suppliers have chosen to ignore Merck’s wishes and offer to sell unapproved MTEP to researchers without permissions. Any reagent supplier that offers MTEP for sale (or has done so in the past) is doing so without license and in breach of patent. The authenticity of any such material is not guaranteed by Merck, nor is the use of any material obtained in this way sanctioned by them.

However, our associates at Merck appreciate the desire from legitimate researchers to obtain small quantities of genuine MTEP directly from them for appropriate laboratory use. Furthermore, in view of Tocris’ relationship with Merck and our continually high ethical standards in respect of licensing matters, Merck has agreed to allow Tocris to partner with them to facilitate this process.

Accordingly, any researcher wishing to obtain genuine MTEP direct from Merck is invited to submit a request for a sample via Tocris2.

Please complete this initial inquiry form, which we will then forward to Merck in confidence.

1See Madey vs Duke, United States Court of Appeals for the Federal Circuit, October 3rd 2002 [Experimental use exception case] etc.

2Following the submission of an initial inquiry, additional information may be required by Merck to allow them to evaluate the appropriateness of providing MTEP in each case.

References:

References:

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. 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. Klodzinska et al (2004) Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABAA signaling. Neuropharmacology 47 342. 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. Brodkin et al (2002) Reduced stress-induced hyperthermia in mGluR5 knockout mice. Eur. J. Neurosci. 16 2241.
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Keywords: MTEP, Glutamate (Metabotropic) Receptors, Potent, Selective MGlu5 Antagonist, Tocris Bioscience

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