Description: mGlu5 antagonist and positive allosteric modulator at mGlu4
Chemical Name: 2-Methyl-6-(2-phenylethenyl)pyridine
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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
Solubility
Soluble 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
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References
References are publications that support the products' biological activity.
Chapmanet 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
Mathiesenet 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
Varneyet al (1999) SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5. J.Pharmacol.Exp.Ther. 290 170 PMID: 10381773
Keywords: SIB 1893, supplier, Positive, allosteric, modulators, mGlu4, mGluR4, mGlu5, mGluR5, antagonist, positive, Group, III, Receptors, Glutamate, Metabotropic, I, SIB1893, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, III, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
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