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The role of metabotropic glutamate receptors in pain perception

Publication at Third Faculty of Medicine |
2011

Abstract

Chronic pain - persistent or intermittent pain lasting at least three months - is pain that lost its original purpose and became disease by itself, affecting quality of life and often complicating even ordinary daily activities. In spite of wide range of available analgesic drugs significant proportion of patients shows resistance to medication which leads to need of novel drugs.

One of possible targets of novel analgesics are metabotropic glutamate receptors. Metabotropic glutamate receptors belong to the Family 3 of heptahelical G-protein coupled receptors together with calcium sensing receptor, pheromone receptors, some taste receptors and GABA-B receptor.

There are 8 types of metabotropic glutamate receptors, which are divided into 3 groups (Group 1: mGluR1 and mGluR5, Group 2: mGluR2 and mGluR3, Group 3: mGluR4, mGluR6-8). Aim of this paper is to give an overview of current knowledge regarding effect of metabotropic glutamate receptors in pain transmission in physiological and sensitised state and show this evidence in context of possible therapeutic usage.

Recently, mGluR5 seems to be the most promising therapeutic target. Further studies and synthesis of novel specific ligands and allosteric modulators can be important for the future of clininal relevance of metabotropic glutamate receptors.