Description: mGlu5 antagonist and positive allosteric modulator at mGlu4 Chemical Name: 2-Methyl-6-(2-phenylethenyl)pyridine Biological Activity Technical Data Solubility Calculators DatasheetsReferences

Biological Activity

A highly selective non-competitive antagonist for the metabotropic glutamate mGlu5 receptor subtype; displays an IC50 value of 0.3 μM  at hmGlu5, compared with > 100 μM at hmGlu1b, hmGlu2, hmGlu6, hmGlu7 and hmGlu8. Centrally active upon systemic administration in vivo. Positive allosteric modulator at mGlu4 receptors.

Technical Data

M. Wt 195.26
Formula C14H13N
Storage Desiccate at +4°C
CAS Number 6266-99-5
PubChem ID 4713
InChI Key QFWCYNPOPKQOKV-UHFFFAOYSA-N
Smiles CC1=NC(C=CC2=CC=CC=C2)=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

SolubilitySoluble to 100 mM in DMSO

Preparing Stock Solutions

The following data is based on the product molecular weight 195.26. 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 5.12 mL 25.61 mL 51.21 mL
5 mM 1.02 mL 5.12 mL 10.24 mL
10 mM 0.51 mL 2.56 mL 5.12 mL
50 mM 0.1 mL 0.51 mL 1.02 mL
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Product Datasheets

Certificate of Analysis / Product Datasheet Safety Datasheet Select another language: English German French Spanish View SDS

References

References are publications that support the products\' biological activity.

Chapman et al (2000) Anticonvulsant activity of two metabotropic glutamate group I antagonists selective for the mGlu5 receptor: 2-methyl-6-(phenylethynyl)-pyridine (MPEP), and (E)-6-methyl-2-styryl-pyridine (SIB 1893). Neuropharmacology 39 1567 PMID: 10854901

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

Varney et al (1999) SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5. J.Pharmacol.Exp.Ther. 290 170 PMID: 10381773


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