Skip to main content
Article thumbnail
Location of Repository

Allosteric Modulators for mGlu Receptors

By F Gasparini and W Spooren

Abstract

The metabotropic glutamate receptor family comprises eight subtypes (mGlu1-8) of G-protein coupled receptors. mGlu receptors have a large extracellular domain which acts as recognition domain for the natural agonist glutamate. In contrast to the ionotropic glutamate receptors which mediate the fast excitatory neurotransmission, mGlu receptors have been shown to play a more modulatory role and have been proposed as alternative targets for pharmacological interventions. The potential use of mGluRs as drug targets for various nervous system pathologies such as anxiety, depression, schizophrenia, pain or Parkinson’s disease has triggered an intense search for subtype selective modulators and resulted in the identification of numerous novel pharmacological agents capable to modulate the receptor activity through an interaction at an allosteric site located in the transmembrane domain. The present review presents the most recent developments in the identification and the characterization of allosteric modulators for the mGlu receptors

Topics: Article
Publisher: Bentham Science Publishers Ltd.
OAI identifier: oai:pubmedcentral.nih.gov:2656819
Provided by: PubMed Central
Download PDF:
Sorry, we are unable to provide the full text but you may find it at the following location(s):
  • http://www.pubmedcentral.nih.g... (external link)
  • Suggested articles

    Citations

    1. (1996). A novel classof antagonists for metabotropic glutamate receptors, 7-(hydroxyimino)cyclopropachromen-1a-carboxylates.
    2. (2005). Metabotropic glutamate II receptor agonists in panic disorder: a double blind clinical trial with LY354740.
    3. (2001). BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity.
    4. (1997). Pharmacology and functions of metabotropic glutamatereceptors.

    To submit an update or takedown request for this paper, please submit an Update/Correction/Removal Request.