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Metabotropic Glutamate GPCR Assays

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Background of Metabotropic Glutamate Receptors

Metabotropic glutamate receptors (mGluRs) are a large family of glutamate receptors that belongs to the G-protein coupled receptor family. mGluRs can be detected in nearly every important region of the human brain. So far, eight different subtypes of mGluRs (mGlu1-8) have been cloned. mGluRs are subdivided into three groups based on their sequence homology, effector coupling, and pharmacology. Group I mGluRs include mGlu 1 and mGlu 5, they can couple with phospholipase C positively. Group II mGluRs include mGlu 2 and mGlu 3, and the others belong to group III mGluRs. They can both couple to adenylate cyclase negatively.

Structure of the Metabotropic Glutamate receptor 1.Fig.1. Structure of the Metabotropic Glutamate receptor 1. (Uniprot ID P23385; obtained from Alphafold)

Distribution and Function of Metabotropic Glutamate Receptors

Metabotropic glutamate receptors are widely distributed throughout the human central nervous (CNS) system and inhibit specifically in discrete synapses of both neurons and glial cells. Their specific distribution locations vary with the group. The activation of group I mGluRs often results in cellular depolarization and increased neuronal excitability. In contrast, group II and group III mGluRs can suppress the release of neurotransmitters.

Subtypes and Mechanisms of Metabotropic Glutamate Receptors

Research on mGluRs and their associated pathways can do great benefit in the treatment of cancer, primary brain tumors, melanoma, and other brain diseases.

Receptor Gene Mechanism Agonists Antagonists

mGluR1

GRM1

  • mGluR1 belongs to group I mGluRs.
  • mGluR1 can couple with Gq/G11 and phospholipase C positively and lead to phosphatidylinositol hydrolysis.
  • (1S,3R)-ACPD
  • (±)-trans-ACPD
  • CHPG
  • (RS)-3,5-DHPG
  • (S)-3,5-DHPG
  • L-Quisqualic acid
  • S-Sulfo-L-cysteine sodium salt
  • ABP 688
  • AIDA
  • DL-AP3
  • AZD 2066
  • AZD 9272
  • CPCCOEt
  • JNJ 16259685
  • LY 367385
  • LY 456236 hydrochloride
  • MPEP hydrochloride
  • MTEP hydrochloride
  • NPS 2390
  • PHCCC

mGluR2

GRM2

  • mGluR2 belongs to group II mGluRs.
  • mGlur2 is primarily coupled to Gi/o proteins and thereby regulates ion channels in the glutamatergic synapse.
  • (1S,3R)-ACPD
  • (±)-trans-ACPD
  • (2R,4R)-APDC
  • L-CCG-l
  • DCG IV
  • LY 354740
  • LY 379268
  • MAP4
  • (RS)-APICA
  • LY 341495
  • Ro 64-5229

mGluR3

GRM3

  • mGluR3 belongs to group II mGluRs.
  • mGlur3 is primarily coupled to Gi/o proteins and thereby regulates ion channels in the glutamatergic synapse.
  • (1S,3R)-ACPD
  • (±)-trans-ACPD
  • (2R,4R)-APDC
  • L-CCG-l
  • DCG IV
  • LY 354740
  • LY 379268
  • MAP4
  • (RS)-APICA
  • LY 341495
  • Ro 64-5229

mGluR4

GRM4

  • mGluR4 belongs to group III mGluRs.

  • mGlur4 is primarily coupled to Gi/o proteins and thereby regulates ion channels in the glutamatergic synapse.

  • ACPT-I
  • L-AP4
  • CPPG
  • LY 341495
  • MAP4
  • MPPG
  • UBP1112

mGluR5

GRM5

  • mGluR5 belongs to group I mGluRs.
  • mGluR5 can couple with Gq/G11 and phospholipase C positively and lead to phosphatidylinositol hydrolysis.
  • (1S,3R)-ACPD
  • (±)-trans-ACPD
  • CHPG
  • (RS)-3,5-DHPG
  • (S)-3,5-DHPG
  • L-Quisqualic acid
  • S-Sulfo-L-cysteine sodium salt
  • ABP 688
  • AIDA
  • DL-AP3
  • AZD 2066
  • AZD 9272
  • CPCCOEt
  • JNJ 16259685
  • LY 367385
  • LY 456236 hydrochloride
  • MPEP hydrochloride
  • MTEP hydrochloride
  • NPS 2390
  • PHCCC

mGluR6

GRM6

  • mGluR6 belongs to group III mGluRs.
  • mGlur6 is primarily coupled to Gi/o proteins and thereby regulates ion channels in the glutamatergic synapse.
  • ACPT-I
  • L-AP4
  • CPPG
  • LY 341495
  • MAP4
  • MPPG
  • UBP1112

mGluR7

GRM7

  • mGluR7 belongs to group III mGluRs.
  • mGlur7 is primarily coupled to Gi/o proteins and thereby regulates ion channels in the glutamatergic synapse.
  • ACPT-I
  • L-AP4
  • AMN 082 dihydrochloride
  • CPPG
  • LY 341495
  • MAP4
  • MPPG
  • UBP1112
  • XAP 044

mGluR8

GRM8

  • mGluR8 belongs to group III mGluRs.
  • mGlur8 is primarily coupled to Gi/o proteins and thereby regulates ion channels in the glutamatergic synapse.
  • ACPT-I
  • L-AP4
  • (S)-3,4-DCPG
  • CPPG
  • LY 341495
  • MAP4
  • MPPG
  • UBP1112

Assay List of Metabotropic Glutamate Receptors

Creative Biolabs can provide a range of assays of metabotropic glutamate receptors. You can choose the assay in the list or contact us for more information:

GRM1 GRM2 GRM3 GRM4 GRM5 GRM6 GRM7 GRM8
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX506 Magic™ Human GRM1 In Vitro cAMP Assay CHO-K1 cAMP Assay
Calcium Flux Assay
S01YF-0722-KX138 Magic™ Human GRM1 In Vitro Calcium Assay, HEK293 HEK293 Calcium Flux Assay
S01YF-0722-KX139 Magic™ Human GRM1 In Vitro Calcium Assay, CHO-K1 CHO-K1 Calcium Flux Assay
Radioligand Binding Assay
S01YF-1122-KX507 Magic™ Human GRM1 In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-0722-KX140 Magic™ Human GRM2 In Vitro Calcium Assay & [35S]GTPγS binding Assay, HEK293-Ga16 HEK293-Ga16 Calcium Assay; [35S]GTPγS binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-0722-KX141 Magic™ Human GRM3 In Vitro Calcium Assay & [35S]GTPγS binding Assay, HEK293-Gα16-EAAC1 HEK293-Gα16-EAAC1 Calcium Assay; [35S]GTPγS binding Assay
S01YF-1122-KX509 Magic™ Human GRM3 In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-0722-KX142 Magic™ Human GRM4 In Vitro Calcium Assay & [35S]GTPγS binding Assay, HEK293-Gα15 HEK293-Gα15 Calcium Assay; [35S]GTPγS binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-0722-KX143 Magic™ Human GRM5 In Vitro Calcium Assay & Binding Assay, HEK293 HEK293 Calcium Assay; Binding Assay
S01YF-1122-KX512 Magic™ Human GRM5 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-0722-KX144 Magic™ Rat GRM5 In Vitro Calcium Assay & Binding Assay, HEK293 HEK293 Calcium Assay; Binding Assay
IP1 Assay
S01YF-1122-KX513 Magic™ Human GRM5 In Vitro IP1 Assay CHO-K1 IP1 Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-0722-KX145 Magic™ Human GRM6 In Vitro Calcium Assay & [35S]GTPγS binding Assay, HEK293-Gα15 HEK293-Gα15 Calcium Assay; [35S]GTPγS binding Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX515 Magic™ Human GRM6 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX516 Magic™ Human GRM7 In Vitro cAMP Assay CHO-K1 cAMP Assay
Calcium Flux Assay
S01YF-0722-KX146 Magic™ Human GRM7 In Vitro Calcium Assay, HEK293-Gα15-EAAC1 HEK293-Gα15-EAAC1 Calcium Flux Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-0722-KX147 Magic™ Human GRM8 In Vitro Calcium Assay, HEK293-Gα15-EAAC1 HEK293-Gα15-EAAC1 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX517 Magic™ Human GRM8 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay

Published Data

Paper Title

Emotional impairment and persistent upregulation of mGlu5 receptor following morphine abstinence: implications of an mGlu5-MOPr interaction

Journal

International Journal of Neuropsychopharmacology

Published 2016
Abstract

Opioid addiction is a complex and multi-occurring brain disease. After withdrawal, it will produce various negative emotional conditions including depression, stress, and anxiety, and trigger patients to seek and take drugs compulsively, making the maintenance of a drug-free state extremely difficult. Classical antidepressant medications have not been shown to be effective in this patient population, so addressing the underlying mechanisms of mood disturbance during withdrawal is critical. Previous studies have reported the important role of metabotropic glutamate receptor 5 in opioid administration and withdrawal drug-seeking behavior, especially the involvement of mGlu5R in the process of drug addiction, however, the role of mGlu5R in regulating mood disturbance during morphine withdrawal is not deeply understood. In this study, the researchers evaluated the emotional and behavioral consequences of morphine withdrawal in mice and the reversal effect of mGlu5R on this depression-like behavior. Differences in mGlu5R binding capacity in the mouse brain. The findings demonstrate a critical role of mGlu5R in the central nervous system in modulating negative emotional states during opioid withdrawal and a possible μ-opioid receptor (MOPr)-mGlu5R interaction.

Result

In the experiment, addiction in mice is promoted by seven-day ascending dosing, and the behavior/emotional changes in mice were evaluated by the elevated maze and forced swimming test after withdrawal. mGlu5R binding was assessed by mGlu5R autoradiography in dosed mice, weaned mice, and MOPr knockout mice. Experimental data show that morphine withdrawal leads to emotional and behavioral deficits in mice, as well as a significant neuroadaptive upregulation of mGlu5R binding in the brain. After treatment with mGlu5R antagonists, depression-nourishing behavior is improved and reversed. The binding of mGlu5R in specific regions in the brain of MOPr knockout mice was increased compared with the control group, suggesting that mGlu5R and MOPr may have direct molecular interactions in specific brain regions, and the upregulation of mGlu5R may be caused by MOPr knockout as a compensation mechanism. These results support the possibility of an association of mGlu5R with opioid withdrawal-related affective disorders and the existence of a region-specific MOPr-mGlu5R interaction in the brain.

Fig.2. Morphine Morphine withdrawal causes changes in mGlu5R binding.withdrawal causes changes in mGlu5R binding. (Zanos, 2016)

Reference

  1. Zanos, P.; et al. Emotional impairment and persistent upregulation of mGlu5 receptor following morphine abstinence: implications of an mGlu5-MOPr interaction. International Journal of Neuropsychopharmacology. 2016, 19(7): 1-10.
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