ChemiScreen™ Membrane Preparation Human Recombinant mGlu2

Species	Host Cells	Protein Target
Human	Chem-1	mGlu2

Species

Host Cells

Protein Target

Human

Chem-1

mGlu2

Description
Catalogue Number	HTS146M
Trade Name	ChemiScreen Chemicon
Description	ChemiSCREEN™ Membrane Preparation Recombinant Human mGLU₂ Metabotropic Glutamate Receptor
Overview	human GRM2 cDNA encoding mGlu₂
Background Information	Glutamate 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 G_αq, whereas group II (mGlu₂ and mGlu₃) and group III (mGlu₄, mGlu₆, mGlu₇, and mGlu₈) negatively couple to the adenylyl cyclase pathway though G_αi (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, mGlu_2/3 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.

Description

Catalogue Number

HTS146M

Trade Name

ChemiScreen
Chemicon

Description

ChemiSCREEN™ Membrane Preparation Recombinant Human mGLU₂ Metabotropic Glutamate Receptor

Overview

human GRM2 cDNA encoding mGlu₂

Background Information

Glutamate 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 G_αq, whereas group II (mGlu₂ and mGlu₃) and group III (mGlu₄, mGlu₆, mGlu₇, and mGlu₈) negatively couple to the adenylyl cyclase pathway though G_αi (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, mGlu_2/3 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.

Product Information
Format	Membranes
Presentation	Liquid 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.

Product Information

Format

Membranes

Presentation

Liquid 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.

Applications
Application	Human mGlu2 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.
Key Applications	Radioligand binding assay GTPγS binding
Application Notes	Radioligand binding assay and GTPγS binding

Applications

Application

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

Key Applications

Radioligand binding assay
GTPγS binding

Application Notes

Radioligand binding assay and GTPγS binding

Biological Information
Entrez Gene Number	NM_000839.2
Entrez Gene Summary	L-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 Class	C
Host Cells	Chem-1
Protein Target	mGlu2
Target Sub-Family	Glutamate (metabotropic)
UniProt Number	Q14416
UniProt Summary	FUNCTION: 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 Conditions	Membranes 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.

Biological Information

Entrez Gene Number

NM_000839.2

Entrez Gene Summary

L-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 Class

Host Cells

Chem-1

Protein Target

mGlu2

Target Sub-Family

Glutamate (metabotropic)

UniProt Number

Q14416

UniProt Summary

FUNCTION: 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 Conditions

Membranes 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.

Product Usage Statements
Quality Assurance	EC50 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.

Product Usage Statements

Quality Assurance

EC50 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 Conditions	Maintain frozen at -70°C for up to 2 years. Do not freeze and thaw.

Storage and Shipping Information

Storage Conditions

Maintain frozen at -70°C for up to 2 years. Do not freeze and thaw.

Packaging Information
Material Size	200 units

Packaging Information

Material Size

200 units

实验耗材

分子生物学试剂

蛋白与免疫学

生化试剂

细胞及检测试剂

色谱及层析

仪器设备

实验服务

办公用品

ChemiScreen™ Membrane Preparation Human Recombinant mGlu2

浏览了该商品的用户最终购买

浏览了该商品的用户还浏览了

重要规格表

我要咨询