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

PubChem ID

3025961

Name

MPEP

Measurement

- IC50

PubChem ID

11840951

Name

L-glutamate

Measurement

877nM - IC50

PubChem ID

3025961

Name

L-Quisqualate

Measurement

83nM - IC50

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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