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Progress toward allosteric ligands of metabotropic glutamate 7 (mGlu7) receptor: 2008–present

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Abstract

Metabotropic glutamate type 7 (mGlu7) receptor is a member of the group III family of mGlu receptors. It is widely distributed in the central nervous system (CNS) and is preferentially expressed on presynaptic nerve terminals where it is thought to play a critical role in modulating normal neuronal function and synaptic transmission, making it particularly relevant in neuropharmacology. The lack of small-molecule mGlu7 ligands with adequate potency, selectivity and drug-like properties has resulted in difficulties in the preclinical validation of mGlu7 modulation in disease models. In the last decade, allosteric modulators of mGlu7 receptors have emerged as valuable tools with good potency, selectivity and physicochemical properties to study and unleash the therapeutic potential of mGlu7 receptors. This review focusses on the medicinal chemistry of mGlu7 receptor allosteric ligands discovered since 2008.

Graphical abstract: Progress toward allosteric ligands of metabotropic glutamate 7 (mGlu7) receptor: 2008–present

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Publication details

The article was received on 17 Oct 2018, accepted on 11 Dec 2018 and first published on 12 Dec 2018


Article type: Review Article
DOI: 10.1039/C8MD00524A
Citation: Med. Chem. Commun., 2019, Advance Article

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    Progress toward allosteric ligands of metabotropic glutamate 7 (mGlu7) receptor: 2008–present

    H. Vázquez-Villa and A. A. Trabanco, Med. Chem. Commun., 2019, Advance Article , DOI: 10.1039/C8MD00524A

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