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Activation of the mGlu₁ metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M₄ muscarinic receptor allosteric modulators.

ABSTRACT: Recent clinical and preclinical studies suggest that selective activators of the M₄ muscarinic acetylcholine receptor have potential as a novel treatment for schizophrenia. M₄ activation inhibits striatal dopamine release by mobilizing endocannabinoids, providing a mechanism for local effects on dopamine signaling in the striatum but not in extrastriatal areas. G protein-coupled receptors (GPCRs) typically induce endocannabinoid release through activation of Gα_q/11-type G proteins whereas M₄ transduction occurs through Gα_i/o-type G proteins. We now report that the ability of M₄ to inhibit dopamine release and induce antipsychotic-like effects in animal models is dependent on co-activation of the Gα_q/11-coupled mGl

SUBMITTER: Yohn SE

PROVIDER: S-EPMC6588501 | biostudies-literature | 2020 Nov

REPOSITORIES: biostudies-literature

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Activation of the mGlu₁ metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M₄ muscarinic receptor allosteric modulators.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Dataset Information

Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Activation of the mGlu₁ metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M₄ muscarinic receptor allosteric modulators.