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HTS146M ChemiSCREEN™ Membrane Preparation Recombinant Human mGLU2 Metabotropic Glutamate Receptor

Human mGlu2 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Host Cell: Chem-1 Uni Prot Number: Q14416 Entrez Gene Number: NM_000839.2
HTS146M
200 units  
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

SpeciesHost CellsProtein Target
Human Chem-1mGlu2
Description
Catalogue NumberHTS146M
Trade Name
  • ChemiScreen
  • Chemicon
DescriptionChemiSCREEN™ Membrane Preparation Recombinant Human mGLU2 Metabotropic Glutamate Receptor
Overviewhuman GRM2 cDNA encoding mGlu2
Background InformationGlutamate is a main excitatory neurotransmitter in the central nervous system, and it plays a role in learning, memory and neurotoxicity. The biological actions of glutamate are mediated by ionotropic and metabotropic glutamate receptors, which are ion channels and GPCRs respectively. Metabotropic glutamate receptors (mGluRs) are members of the class 3 G-protein coupled receptor family, which are characterized by a large extracellular domain. They are further classified into group I, II, and III mGluRs on the basis of their sequence identity, pharmacology, and signal transduction mechanism. Group I (mGlu1 and mGlu5) couple to the phospholipase C pathway through Gαq, whereas group II (mGlu2 and mGlu3) and group III (mGlu4, mGlu6, mGlu7, and mGlu8) negatively couple to the adenylyl cyclase pathway though Gαi (Conn and Pin, 1997). Agonists of the Group II metabotropic glutamate receptors, mGlu2 and mGlu3, display efficacy in animal models of anxiety and psychosis. A key role for mGlu2 in mediating these effects is indicated by the observation that selective allosteric potentiator of mGlu2 also retains antipsychotic-like activities in mice (Galici et al., 2005). In addition, mGlu2/3 agonists display analgesic activity in animal models (Jones et al., 2005). Chemicon's mGlu2 membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression; thus, they are ideal HTS tools for screening of mGlu2 interactions with its ligands. The cell line exhibits a calcium response with EC50s of 0.51uM, 5.6uM, and 8.3uM for DCG IV, (2R4R) APDC, and glutamate. The membrane preparations exhibit EC50s of of 0.72uM, 5.07uM, and 6.29uM for DCG IV, (2R4R) APDC, and glutamate in a GTPγS binding assay.
References
Product Information
FormatMembranes
HS Code3822 19 90
PresentationLiquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives.
Packaging method: Membrane protein was adjusted to 1 mg/ml in packaging buffer, rapidly frozen, and stored at -80°C.
Quality LevelMQ100
Applications
ApplicationHuman mGlu2 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.
Key Applications
  • Radioligand binding assay
  • GTPγS binding
Application NotesRadioligand binding assay and GTPγS binding
Biological Information
Entrez Gene Number
Entrez Gene SummaryL-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.
Gene Symbol
  • GRM2
  • mGlu2
  • GPRC1B
  • MGLUR2
  • mGluR2
  • GLUR2
GPCR ClassC
Host CellsChem-1
Protein TargetmGlu2
Target Sub-FamilyGlutamate (metabotropic)
UniProt Number
UniProt SummaryFUNCTION: SwissProt: Q14416 # Receptor for glutamate. The activity of this receptor is mediated by a G-protein that inhibits adenylate cyclase activity. May mediate suppression of neurotransmission or may be involved in synaptogenesis or synaptic stabilization.
SIZE: 872 amino acids; 95568 Da
SUBUNIT: Interacts with GRASP (By similarity).
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
TISSUE SPECIFICITY: Widely expressed in different regions of the adult brain as well as in fetal brain.
SIMILARITY: SwissProt: Q14416 ## Belongs to the G-protein coupled receptor 3 family.
Incubation ConditionsMembranes are permeabilized by addition of saponin to an equal concentration by mass, then mixed with [35S]-GTPγS (final concentration of 0.1 nM) in 20 mM HEPES, pH 7.4/100 mM NaCl/10 mM MgCl2/0.5 µM GDP in a nonbinding 96-well plate. Unlabeled DCG IV, (2R4R) APDC, and glutamate are added to the final concentration indicated in Figure 1 (final volume 100 µL), and incubated for 30 min at 30°C. The binding reaction is transferred to a GF/B filter plate (Millipore MAHF B1H) previously prewetted with water, and washed 3 times (1 mL per well per wash) with cold 10 mM sodium phosphate, pH 7.4. The plate is dried and counted.

One vial contains enough membranes for at least 200 assays (units), where one unit is the amount of membrane that will yield greater than 1000 cpm specific DCG IV, (2R4R) APDC, or glutamate -stimulated [35S]-GTPγS binding.
The mGlu2 membrane preparation is expected to be functional in a radioligand binding assay; however, the end user will need to determine the optimal radiolabeled ligand for use with this product.
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Quality AssuranceEC50 in GTPγS binding assay by Glutamate: ~ 6.29 μM
EC50 in GTPγS binding assay by (2R4R) APDC: ~ 5.07 μM
EC50 in GTPγS binding assay by DCG IV: ~ 0.72 μM
Usage Statement
  • Unless otherwise stated in our catalog or other company documentation accompanying the product(s), our products are intended for research use only and are not to be used for any other purpose, which includes but is not limited to, unauthorized commercial uses, in vitro diagnostic uses, ex vivo or in vivo therapeutic uses or any type of consumption or application to humans or animals.
Storage and Shipping Information
Storage ConditionsMaintain frozen at -70°C for up to 2 years. Do not freeze and thaw.
Packaging Information
Material Size200 units
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
HTS146M 04053252581649

Documentation

ChemiSCREEN™ Membrane Preparation Recombinant Human mGLU2 Metabotropic Glutamate Receptor SDS

Title

Safety Data Sheet (SDS) 

ChemiSCREEN™ Membrane Preparation Recombinant Human mGLU2 Metabotropic Glutamate Receptor Certificates of Analysis

TitleLot Number
CHEMISCREEN TM MEMBRANE PREPARATION RECOMBINANT HU mGLU2 METOBOTROPIC GLUTAMATE RECEPTOR - SC281836 SC281836
CHEMISCREENTM MEMBRANE PREPARATION SC032215
CHEMISCREENTM MEMBRANE PREPARATION RECOMBINANT HUMAN mGLU2 METABOTROPIC GLUTAMATE RECEPTOR - 2377141 2377141
CHEMISCREENTM MEMBRANE PREPARATION RECOMBINANT HUMAN mGLU2 METABOTROPIC GLUTAMATE RECEPTOR - SC944259 SC944259
CHEMISCREENTM MEMBRANE PREPARATION RECOMBINANT HUMAN mGLU2 METABOTROPIC GLUTAMATE RECEPTOR - 2089082 2089082
CHEMISCREENTM MEMBRANE PREPARATION RECOMBINANT HUMAN mGLU2 METABOTROPIC GLUTAMATE RECEPTOR - 2326018 2326018
CHEMISCREEN™ MEMBRANE PREPARATION RECOMBINANT HUMAN mGLU2 METABOTROPIC GLUTAMATE RECEPTOR -SC733621 SC733621
CHEMISCREEN™ MEMBRANE PREPARATION RECOMBINANT HUMAN mGLU2 METABOTROPIC GLUTAMATE RECEPTOR - SC113865 SC113865

References

Reference overviewPub Med ID
A selective allosteric potentiator of metabotropic glutamate (mGlu) 2 receptors has effects similar to an orthosteric mGlu2/3 receptor agonist in mouse models predictive of antipsychotic activity
Galici, Ruggero, et al
J Pharmacol Exp Ther, 315:1181-7 (2005)  2005

16123306 16123306
Analgesic effects of the selective group II (mGlu2/3) metabotropic glutamate receptor agonists LY379268 and LY389795 in persistent and inflammatory pain models after acute and repeated dosing
Jones, Carrie K, et al
Neuropharmacology, 49 Suppl 1:206-18 (2005)  2005

15998527 15998527
Pharmacology and functions of metabotropic glutamate receptors.
Conn, P J and Pin, J P
Annu. Rev. Pharmacol. Toxicol., 37: 205-37 (1997)  1997

Show Abstract 		9131252 9131252

Brochure

Title
Pathways and Biomarkers of Glutamatergic Synapse Flyer

Data Sheet

Title
CHEMISCREEN MEMBRANE PREPARATION RECOMBINANT HUMAN mGLU2 METABOTROPIC GLUTAMATE RECEPTOR

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