Biological Activity
Potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw. Also available as part of the Group I mGlu Receptor Tocriset™.
Compound Libraries
MPEP hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 229.71 |
| Formula | C14H11N.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 219911-35-0 |
| PubChem ID | 9794588 |
| InChI Key | PKDHDJBNEKXCBI-UHFFFAOYSA-N |
| Smiles | Cl.CC1=CC=CC(=N1)C#CC1=CC=CC=C1 |
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 | 22.97 | 100 | |
| ethanol | 22.97 | 100 | |
| water | 1.15 | 5mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 229.71. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4.35 mL | 21.77 mL | 43.53 mL |
| 5 mM | 0.87 mL | 4.35 mL | 8.71 mL |
| 10 mM | 0.44 mL | 2.18 mL | 4.35 mL |
| 50 mM | 0.09 mL | 0.44 mL | 0.87 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Gasparini et al (1999) 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology 38 1493 PMID: 10530811
Mathiesen et al (2003) Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP. Br.J.Pharmacol. 138 1026 PMID: 12684257
Salt et al (1999) Antagonism of the mGlu5 agonist 2-chloro-5-hydroxyphenylglycine by the novel selective mGlu5 antagonist 6-methyl-2-(phenylethynyl)-pyridine (MPEP) in the thalamus. Br.J.Pharmacol. 127 1057 PMID: 10455248
Bowes et al (1999) Anti-hyperalgesic effects of the novel metabotropic glutamate receptor 5 antagonist, methylphenylethynylpyridine, in rat models of inflammatory pain. Br.J.Pharmacol. 126 250P PMID:
Keywords: MPEP hydrochloride, supplier, mGlu5, mGluR5, antagonists, positive, allosteric, modulators, mGlu4, mGluR4, PAM, Positive, Group, I, Receptors, Glutamate, Metabotropic, III, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, III, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
