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.
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
Organism:
Human
Construct Details:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[3H]Quisqualate
Ligand Kd (nM):
44
Ligand Concentration:
40nM
Non Specific:
1 mM L-Glutamate
Incubation:
120 min at RT
Control Inhibitor:
L-Quisqualate
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.
Test Sample Requirements:
Minimum for 1) Screen: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 μl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
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:
France - Celle L'Evescault
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