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Methylphenylethynylpyridine (MPEP) Novartis.

F Micheli1

  • 1Glaxo Wellcome, Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy. fm20244@glaxowellcome.co.uk

Current Opinion in Investigational Drugs (London, England : 2000)
|March 16, 2001
PubMed
Summary

Researchers explored metabotropic glutamate receptor 5 (mGluR5) antagonists for neurological conditions. Methylphenylethynylpyridine (MPEP) showed significant potential in treating inflammatory pain by reversing hyperalgesia.

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Excitatory amino acid receptors, including metabotropic glutamate receptor 5 (mGluR5), are implicated in various neurological disorders.
  • SIBIA and Novartis investigated mGluR5 antagonists for potential therapeutic applications.

Purpose of the Study:

  • To identify and characterize selective mGluR5 antagonists for treating conditions like epilepsy, stroke, anxiety, pain, and neurodegenerative diseases.
  • To evaluate the efficacy of novel compounds, particularly Methylphenylethynylpyridine (MPEP), in preclinical models.

Main Methods:

  • Development of a series of mGluR5 antagonists, including SIB-1893, SIB-1757, and MPEP.
  • In vitro assays to determine receptor binding affinity and selectivity (e.g., IC50 for mGluR5).
  • In vivo studies using animal models of inflammatory pain (e.g., Freund's complete adjuvant model).

Main Results:

  • MPEP was identified as a potent, selective, and systemically active noncompetitive mGluR5 antagonist with an IC50 of 12 nM.
  • MPEP demonstrated no cross-reactivity with other glutamate receptors up to 100 microM.
  • Oral administration of MPEP (100 mg/kg) resulted in a 70% reversal of mechanical hyperalgesia in an inflammatory pain model.

Conclusions:

  • mGluR5 plays a significant role in inflammatory mechanical hyperalgesia.
  • MPEP is a promising lead compound for the development of novel analgesics targeting mGluR5.
  • Further investigation into MPEP and related compounds is warranted for neurological and pain management therapies.

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