Group II metabotropic glutamate receptor (mGluR2/3) agonists have strong activity in a series of animal models that predict the activity of antianxiety and antipsychotic drugs. These exciting findings represent a breakthrough and may eventually lead to the introduction of mGluR2/3 agonists as a new treatment for anxiety and/or schizophrenia.
Introduction to mGluR2/3
Group II metabotropic glutamate receptors (mGluR2 and mGluR3) are distributed in brain regions related to social behavior and emotional regulation, such as the prefrontal cortex, anterior cingulate cortex, thalamus, amygdala and hippocampus. mGluR2 and mGluR3 are also found in postsynaptic and glial cells, although they are mainly located in presynaptic region, where they act as their own and heterogenous receptors and inhibit the release of glutamate and other neurotransmitters. mGluR2/3 agonists have shown promise as non-dopaminergic antipsychotics because they alleviate symptoms of schizophrenia in both animal models and human patients.
Function of mGluR2/3 Agonist in Schizophrenia
GABAergic interneurons in the central nervous system are activated by the axonal collateral branches of excitatory neurons and produce strong inhibitory feedback to these excitatory cells. According to the hypothesis of N-methyl-D-aspartate (NMDA) dysfunction, hyperglutamatemia is due to the decreased effect of NMDA receptor on GABAergic neurons, which reduces the inhibitory control of excitatory pyramidal neurons, resulting in increased glutamate release and overexpression of glutamatergic receptors. This eventually leads to excitotoxicity damage and cognitive impairment. mGluR2/3 agonists can reduce the presynaptic glutamate release of excitatory neurons, and then reverse hyperglutamatemia, thereby reducing the symptoms of schizophrenia patients.
mGluR2/3 Agonist Development Services at Creative Biolabs
In particular, compared with other typical and atypical antipsychotics, patients using mGluR2/3 agonists did not exhibit side effects and low tolerance associated with current dopaminergic antipsychotics. Therefore, selective mGluR2/3 agonists and mGluR2/3 positive allosteric modulators (PAMs) are still considered as promising candidates for pharmacogenomic therapy, or as an adjunct to antipsychotic drugs for schizophrenia, especially for cognitive and negative symptoms.
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