Metabotropic glutamate receptor 7 is a

protein Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residues. Proteins perform a vast array of functions within organisms, including catalysing metabolic reactions, DNA replication, respo ...

that in humans is encoded by the ''GRM7''

gene In biology, the word gene (from , ; "...Wilhelm Johannsen coined the word gene to describe the Mendelian units of heredity..." meaning ''generation'' or ''birth'' or ''gender'') can have several different meanings. The Mendelian gene is a ba ...

Function

L-glutamate Glutamic acid (symbol Glu or E; the ionic form is known as glutamate) is an α-amino acid that is used by almost all living beings in the biosynthesis of proteins. It is a non-essential nutrient for humans, meaning that the human body can synt ...

is the major excitatory

neurotransmitter A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a synapse. The cell receiving the signal, any main body part or target cell, may be another neuron, but could also be a gland or muscle cell. Neuro ...

in the central nervous system and activates both ionotropic and

metabotropic glutamate receptor The metabotropic glutamate receptors, or mGluRs, are a type of glutamate receptor that are active through an indirect metabotropic process. They are members of the group C family of G-protein-coupled receptors, or GPCRs. Like all glutamate rece ...

s. 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 AMN082 (''N'',''N′''-dibenzhydrylethane-1,2-diamine) is a selective metabotropic glutamate receptor 7 (mGluR7) allosteric agonist. It mimics the effect of glutamate. AMN082 is the first selective mGluR7 agonist and has expanded the poten ...

allosteric In biochemistry, allosteric regulation (or allosteric control) is the regulation of an enzyme by binding an effector molecule at a site other than the enzyme's active site. The site to which the effector binds is termed the ''allosteric site ...

agonist; induces rapid

internalization Internalization ( or internalisation) is the process of making something internal, with more specific meanings in various fields. It is the opposite of externalization. Psychology and sociology In psychology, internalization is the outcome of ...

; non-glutamatergic binding component *

LSP2-9166 LSP2-9166 is a drug which acts as a selective agonist for the group III metabotropic glutamate receptors, with a reasonably potent EC50 of 70nM at mGluR4 and 220nM at mGluR7, and weaker activity of 1380nM at mGluR6 and 4800nM at mGluR8. It has ...

: mixed agonist at mGluR₄ and mGluR₇

Antagonists

MMPIP MMPIP is a drug used in scientific research that acts as a selective antagonist for the metabotropic glutamate receptor subtype mGluR7. This receptor subtype appears to be involved in the downstream response to cocaine Cocaine (from , f ...

: allosteric antagonist/inverse agonist *

XAP044 XAP044 is a drug which acts as a potent and selective antagonist of the metabotropic glutamate receptor 7 (mGluR7). It inhibits long-term potentiation in the amygdala and inhibits responses associated with stress and anxiety Anxiety is an emo ...

Negative allosteric modulators

ADX71743 ADX71743 is a drug which acts as a potent and selective negative allosteric modulator of the metabotropic glutamate receptor 7. Few selective ligands are available for this receptor, and so ADX71743 has played an important role into scientific res ...

Interactions

Metabotropic glutamate receptor 7 has been shown to

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with

PICK1 Protein Interacting with C Kinase - 1 is a protein that in humans is encoded by the ''PICK1'' gene. Function The protein encoded by this gene contains a PDZ domain, through which it interacts with protein kinase C, alpha ( PRKCA). This protein ...

Clinical

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