Methoxy-PEPy is a potent, selective mGlu5 receptor antagonist with IC50 of 1 nM.
Methoxy-PEPy exhibits 14-fold higher binding in forebrain relative to cerebellum in mGlu5 receptor-deficient mice.
The radioligand [3H]methoxy-PEPy is useful for determining the occupancy of mGlu5 receptors in the brain.
Physicochemical Properties
M.Wt
210.2313
Formula
C13H10N2O
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
Pyridine, 3-methoxy-5-[2-(2-pyridinyl)ethynyl]-
References
1. Cosford ND, et al. Bioorg Med Chem Lett. 2003 Feb 10;13(3):351-4.
2. Anderson JJ, et al. Eur J Pharmacol. 2003 Jul 18;473(1):35-40.
3. Salisbury BG, et al. Eur J Pharmacol. 2008 Jan 28;579(1-3):34-9.
4. Hellyer SD, et al. Mol Pharmacol. 2018 Mar 7. pii: mol.117.111518.
