Biological Information

Background Information:

Glutamate is the major excitatory transmitter in the mammalian central nervous system. The receptor amino acid sequences lie in the same superfamily as GABA, glycine, serotonin 5-HT3 and nicotinic acetylcholine, within the general class of ligand-gated ion channels. Glutamate receptors are classified functionally as ligand-gated ion channels (“ionotropic”) or as “metabotropic” receptors (mGluR) coupled via GTP-binding proteins. The eight known members of the mGluR subfamily have been divided into three groups on the basis of their sequence identity, pharmacology, and preferred signal transduction mechanism. Group I (mGluRs 1 and 5) signal through inositol phospholipid breakdown whereas Group II (mGluRs 2 and 3) and Group III (mGluRs 4, 6 ,7 and 8) inhibit adenylyl cyclase.

DiscoverX® Calcium cell lines overexpress naturally Gq coupled, wildtype GPCRs and are designed to detect calcium mobilization in response to agonist stimulation of the receptor. Signal can be detected using the Calcium No WashPLUS Detection Kit.

Family:

GPCR

Sub Family:

Glutamate (Metabotropic)

Class:

Class C

Protein Name:

mGlu5

Uniprot Number:

P41594

Protein Aliases:

protein phosphatase 1, regulatory subunit 86

Gene Name:

GRM5

Gene ID:

2915

Gene Aliases:

MGLUR5|GPRC1E|mGlu5|PPP1R86

Accession Number:

NM_000842.3

Organism:

Human

Cell Type:

U2OS

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

PAM

Testing Information

Control Activator:

L-glutamate

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 10 concentrations are selected

Test Sample Requirements:

40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)

Minimum Order Quantity:

20

Turnaround Time

Standard:

15 Business Days

Clinical Relevance

Adverse / Beneficial Action:

It has been suggested that the group I receptor mGlu5 antagonists may be useful in the treatment of a a number of disease states, including chronic pain, various psychiatric and neurological disorders, substance abuse and withdrawal, obesity and gastroesophageal reflux disease (GERD).

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA