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 Family	Receptor	Species	Parental	Stable Cell Lines	Division-Arrested Cells	Membranes
Metabotropic Glutamate	mGlu1	human	CHO-K1	C1188-1	DC1188-1	MC1188-1
	mGlu2	human	HEK293T	C1189a	DC1189a	MC1189a
	mGlu2	human	HEK293T Gqi5	HG1189Gi	DHG1189Gi	MHG1189Gi
	mGlu2	human	HEK293T Gαqi5	HG1189	HG1189	HG1189
	mGlu2	human	HEK293T Gαqi5	HG1189a	HG1189a	HG1189a
	mGlu2	rat	HEK293T Gαqi5	HGr1189b	DHGr1189b	MHGr1189b
	mGlu3	human	HEK293T Gαqi5	CG1190	DCG1190	MCG1190
	mGlu4	dog	CHO-K1 Gαqi5	HGd1191-1	DHGd1191-1	MHGd1191-1
	mGlu4	human	HEK293T	C1191a	DC1191a	MC1191a
	mGlu4	human	HEK293T Gαqi5	CG1191	DCG1191	MCG1191
	mGlu4	mouse	CHO-K1 Gαqi5	HGm1191-1a	DHGm1191-1a	MHGm1191-1a
	mGlu4	mouse	CHO-K1 Gαqi5	HGm1191-1b	DHGm1191-1b	MHGm1191-1b
	mGlu4	mouse	CHO-K1 Gαqi5	HGm1191-1c	DHGm1191-1c	MHGm1191-1c
	mGlu4	mouse	CHO-K1 Gαqi5	HGm1191-1d	DHGm1191-1d	MHGm1191-1d
	mGlu4	rat	HEK293T	Cr1191	DCr1191	MCr1191
	mGlu4	human	HEK293T Gαqi5	CG1191a	DCG1191a	MCG1191a
	mGlu5	human	HEK293T	C1192	DC1192	MC1192
	mGlu5	human	HEK293T B-ARRESTIN2	CA1192BA2	DCA1192BA2	MCA1192BA2
	mGlu6	human	HEK293T	C1193	DC1193	MC1193
	mGlu6	human	HEK293T Gαqi5	CG1193	DCG1193	MCG1193
	mGlu7	human	HEK293T	C1194	DC1194	MC1194
	mGlu7	human	HEK293T Gαqi5	CG1194	DCG1194	MCG1194
	mGlu8	human	HEK293T	C1195	DC1195	MC1195
	mGlu8	human	HEK293T	C1195a	DC1195a	MC1195a
	mGlu8	human	HEK293T Gαqi5	CG1195	DCG1195	MCG1195
	mGlu8	human	CHO-K1	C1195-1a	DC1195-1a	MC1195-1a