Metabotropic Glutamate GPCR Family Subtypes and Products

What Are Metabotropic Glutamate Receptors?

Metabotropic glutamate (mGlu) receptors are a family of G protein-coupled receptors (GPCRs) comprised of three receptor groups: Group-I (mGlu1 and mGlu5), Group-II (mGlu2 and mGlu3), and Group-III (mGlu4, mGlu6, mGlu7, and mGlu8). Metabotropic glutamate receptors are found in hippocampal and cerebellar neurons, and play a role in various nervous system functions, such as anxiety, learning, memory, and pain. mGlu receptors are being heavily researched, and are already being used for therapeutic applications in the treatment of various diseases. mGlu2 and mGlu3 agonists were proven effective in the treatment of generalized anxiety disorder, and another agonist, Eglumegad, shows promise of being an effective schizophrenia treatment. mGlu4 agonists also show potential for the treatment of Parkinson’s disease.

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Metabotropic Glutamate Receptor Information

Clickable Text Interaction

mGlu1

mGlu2

mGlu3

mGlu4

mGlu5

mGlu6

mGlu7

mGlu8

The neurotransmitter L-glutamate interacts with both ionotropic and metabotropic receptors. The metabotropic glutamate receptors (mGluRs), which are G protein-coupled receptors, have been divided into 3 groups on the basis of sequence homology, putative signal transduction mechanisms, and pharmacologic properties. Group II and group III mGluRs are linked to the inhibition of the cyclic AMP cascade, but differ in their agonist selectivity.

The mGluR2 is a member of group II metabotropic glutamate receptors.

Metabotropic glutamate receptor mGluR3 is a G protein-coupled receptor for glutamate. Glutamate is the major excitatory neurotransmitter in the mammalian central nervous system and functions to regulate excitability via pre- and postsynaptic mechanisms. The mGluR3 receptor is widely expressed in glial cells but also shows discrete localization both pre- and postsynaptic on glutamatergic and other neurotransmitter synapses. It is also expressed within forebrain regions including hippocampus and thalamus. Agonists of mGluR3 have been shown to suppress enhanced glutamatergic excitations in brain synapses known to be involved in the expression of fear/anxiety in animals and humans. It is anticipated that mGluR3 receptor represent a promising new target for treatment of anxiety and stress-related disorders in humans.

L-glutamate is the major excitatory neurotransmitter in the central nervous system and activates both ionotropic and metabotropic glutamate receptors. The metabotropic glutamate receptors (mGluRs), which are G protein-coupled receptors, have been divided into 3 groups on the basis of sequence homology, putative signal transduction mechanisms, and pharmacologic properties. Group II and group III mGluRs are linked to the inhibition of the cyclic AMP cascade, but differ in their agonist selectivity. Group III agonists include L-2-amino-4-phosphonobutyrate (L-AP4) and L-serine-O-phosphate (Wu et al., 1998).

mGluR5 is a member of Group I. It mainly expresses the brain although its precise role in various cortical functions remains unclear.

mGluR6 is a member of Group III. It mainly expresses in on-bipolar cells in retina.

mGluR7 is a member of Group III. Immunohistochemistry and in situ hybridization showed that mGluR7 expresses in various sites in the nervous system.

The human mGluR8 protein shares 67 to 70% sequence similarity with mGluR4 and mGluR7 and 99% amino acid identity with mouse mGluR8.

Metabotropic Glutamate Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
Metabotropic GlutamatemGlu1humanCHO-K1C1188-1DC1188-1MC1188-1
mGlu2humanHEK293TC1189aDC1189aMC1189a
mGlu2humanHEK293T Gqi5HG1189GiDHG1189GiMHG1189Gi
mGlu2humanHEK293T Gαqi5HG1189HG1189HG1189
mGlu2humanHEK293T Gαqi5HG1189aHG1189aHG1189a
mGlu2ratHEK293T Gαqi5HGr1189bDHGr1189bMHGr1189b
mGlu3humanHEK293T Gαqi5CG1190DCG1190MCG1190
mGlu4dogCHO-K1 Gαqi5HGd1191-1DHGd1191-1MHGd1191-1
mGlu4humanHEK293TC1191aDC1191aMC1191a
mGlu4humanHEK293T Gαqi5CG1191DCG1191MCG1191
mGlu4mouseCHO-K1 Gαqi5HGm1191-1aDHGm1191-1aMHGm1191-1a
mGlu4mouseCHO-K1 Gαqi5HGm1191-1bDHGm1191-1bMHGm1191-1b
mGlu4mouseCHO-K1 Gαqi5HGm1191-1cDHGm1191-1cMHGm1191-1c
mGlu4mouseCHO-K1 Gαqi5HGm1191-1dDHGm1191-1dMHGm1191-1d
mGlu4ratHEK293TCr1191DCr1191MCr1191
mGlu4humanHEK293T Gαqi5CG1191aDCG1191aMCG1191a
mGlu5humanHEK293TC1192DC1192MC1192
mGlu5humanHEK293T B-ARRESTIN2CA1192BA2DCA1192BA2MCA1192BA2
mGlu6humanHEK293TC1193DC1193MC1193
mGlu6humanHEK293T Gαqi5CG1193DCG1193MCG1193
mGlu7humanHEK293TC1194DC1194MC1194
mGlu7humanHEK293T Gαqi5CG1194DCG1194MCG1194
mGlu8humanHEK293TC1195DC1195MC1195
mGlu8humanHEK293TC1195aDC1195aMC1195a
mGlu8humanHEK293T Gαqi5CG1195DCG1195MCG1195
mGlu8humanCHO-K1C1195-1aDC1195-1aMC1195-1a

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