Metabotropic glutamate receptor 7

Metabotropic glutamate receptor 7 is a protein that in humans is encoded by the GRM7 gene.

Function

L-glutamate is the major excitatory neurotransmitter in the central nervous system and activates both ionotropic and metabotropic glutamate receptors. Glutamatergic neurotransmission is involved in most aspects of normal brain function and can be perturbed in many neuropathologic conditions. The metabotropic glutamate receptors are a family of G protein-coupled receptors, that have been divided into 3 groups on the basis of sequence homology, putative signal transduction mechanisms, and pharmacologic properties. Group I includes GRM1 and GRM5 and these receptors have been shown to activate phospholipase C. Group II includes GRM2 and GRM3 while Group III includes GRM4, GRM6, GRM7 and GRM8. Group II and III receptors are linked to the inhibition of the cyclic AMP cascade but differ in their agonist selectivities. Alternative splice variants of GRM8 have been described but their full-length nature has not been determined.

Glutamate has lower affinity for mGluR7 than the other metabotropic glutamate receptors and it has been suggested that mGluR7 may have a regulatory role to dampen the effects of excessive glutamate levels.

Ligands

Agonists

• AMN082: allosteric agonist; induces rapid internalization; non-glutamatergic binding component

• LSP2-9166: mixed agonist at mGluR₄ and mGluR₇

Antagonists

• MMPIP: allosteric antagonist/inverse agonist
• XAP044

Negative allosteric modulators

• ADX71743

Interactions

Metabotropic glutamate receptor 7 has been shown to interact with PICK1.

Clinical

Mutations in both copies have been associated with developmental and epileptic encephalopathy, microcephaly, hypomyelination and cerebral atrophy.

Further reading

Template:PDB Gallery Template:Metabotropic glutamate receptor modulators This article incorporates text from the United States National Library of Medicine, which is in the public domain.