Overview

  • Product name
    MPEP hydrochloride, mGlu5 antagonist
  • Description
    Potent, selective mGlu5 antagonist
  • Biological description
    Subtype selective and potent non-competitive mGlu5 antagonist (IC50 = 36 nM). Central effects following systemic administration in vivo.
  • Purity
    > 99%
  • CAS Number
    96206-92-7
  • Chemical structure
    Chemical Structure

Properties

Images

  • Basal PLD activity is strongly stimulated by the D1/5R agonist and blocked by the D1/5R, mGluR5, mGluR1, and the PLD-linked mGluR antagonists in the amygdala of cocaine CPP animals.
    The dotted line indicates PLD activity associated with control slices (no EtOH added) which was determined for each animal and used to calculate the change in PLD activity levels with EtOH and/or drug application.

  • Astrocyte Ca2+ signal inhibition does not affect interictal discharges. (A–D) Mean percentage of astrocytes activated by the ictal discharges (A), mean duration (B) and frequency (C) of the ictal discharge, and mean frequency of interictal discharges (D) under different experimental conditions in EC slice preparations. Controls (n=16), MPEP (ab120008) (n=7), PPADS (ab120009) (n=9), and MPEP+PPADS (n=3). A single asterisk (*) indicates p<0.05; double asterisks (**), p<0.01.
  • Ca2+ signal from a field A neuron, a field B neuron, and field A astrocytes in response to repetitive episodes of NMDA stimulation (black arrowheads). The NMDA stimulation that evoked an ictal discharge became ineffective after blocking the astrocyte response by bath perfusion with MPEP (ab120008) and PPADS (ab120009). An ictal discharge could be recovered by increasing the number of NMDA puffs (white arrowheads). A double NMDA pulse evoked both astrocyte activation and the ictal discharge after inhibitor washout.

References

This product has been referenced in:
  • Malherbe P  et al. Mutational analysis and molecular modeling of the binding pocket of the metabotropic glutamate 5 receptor negative modulator 2-methyl-6-(phenylethynyl)-pyridine. Mol Pharmacol 64:823-32 (2003). Read more (PubMed: 14500738) »
  • Salt TE  et al. 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 127:1057-9 (1999). Read more (PubMed: 10455248) »
  • Gasparini F  et al. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology 38:1493-503 (1999). Read more (PubMed: 10530811) »
See all 27 Publications for this product

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