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. 2007 Sep;5(3):187-94.
doi: 10.2174/157015907781695900.

Allosteric modulators for mGlu receptors

F Gasparini  1 , W Spooren
Affiliations

Allosteric modulators for mGlu receptors

F Gasparini et al. Curr Neuropharmacol. 2007 Sep.

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.

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Figures

Fig. (1)
Fig. (1)
Group I mGluRs signal transduction pathway.
Fig. (2)
Fig. (2)
Group II and III mGluR signal transduction pathway.
Fig. (3)
Fig. (3)
mGluR1 allosteric modulators.
Fig. (4)
Fig. (4)
mGluR5 allosteric modulators.
Fig. (5)
Fig. (5)
mGluR2 allosteric modulators.
Fig. (6)
Fig. (6)
Group III allosteric modulators.
See this image and copyright information in PMC

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