MGluR5, MPEP

Paterson, N.E., Semenova, S., Gasparini, F., Markou, A. The mGluR5 antagonist MPEP decreased nicotine self-administration in rats and mice. Psychopharmacology (Berlin). 167 257, 2003. 

Bespalov, A.Y., Dravolina, O.A., Sukhanov, I. et al. Metabotropic glutamate receptor (mGluR5) antagonist MPEP attenuated cue- and schedule-induced reinstatement of nicotine self-administration behavior in rats. Neuropharmacology. 49(Suppl.) 167, 2005. 

Fig. 8. Allosteric sites in the mGluR 7TM. The chemical structures of the allosteric inhibitors MPEP, EM-TBPC, BAY36-7620, and CPCCOEt, and the allosteric potentiator Ro 67-7476 are given. The crucial residues or regions for the subtype selectivity of each of the compounds are stated and shown in a schematic illustration of the mGluRl 7TM viewed from the extracellular side of the cell membrane. The residues in mGluRl corresponding to those involved in MPEP binding to mGluR5 are also shown in the illustration.

MPEP, selective mGluR5 antagonist, 2-Methyl-6-phenyl-ethynyl-pyridine... 

Fig. 11 Negative allosteric modulators (non-MPEP-based) of mGluR5...

Rodriguez AL, Williams R, Zhou Y et al (2009) Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype. Bioorg Med Chem Lett 19 3209-3213... 

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