PrecisION hGluR6-HEK Recombinant Cell Line

PrecisION hGluR6-HEK Recombinant Cell Line

Upstate (Millipore)

2 mL

Recombinant HEK293 cell line expressing human GluR6.

hGluR6 is a member of the ligand-gated, kainate family of glutamate receptors also known as GRIK2. It can form both hetero and homo-tetrameric, cation permeable, channels and is expressed at high levels in the hippocampus and striatum of the CNS. Pre- and postsynaptic kainate receptors are able to regulate both neurotransmitter release and excitability in a synapse-specific manner. GRIK2 has been implicated in a range of neurophysiological conditions such as autism, obsessive compulsive disorder, as well as disease states e.g. Schizophrenia, epilepsy and Huntingdon’s disease.

HEK293 cells expressing hGRIK2 were characterized in terms of their pharmacological and biophysical properties using whole-cell patch clamp techniques. The mean current amplitude in response to the application of 100 μM kainate was 671.5 + 73.3 pA (mean + SEM; holding potential -60 mV). The EC₅₀ value for kainate derived from a dose-response (n=2-4 cells per concentration) was 39.8 μM. The pharmacology of the hGRIK2-HEK293 cell line was also examined by calcium flux assay on the FLIPR system. Four known GRIK2 agonists (glutamate, kainate, SYM2081 and domate) were used to evaluate the cell line. pEC50 values were in line with data previously reported using the FLIPR system. The standard antagonists CNQX (6-cyano-7-nitroquinoxaline-2,3-dione) and NBQX (3-dihydroxy-6-nitro-7-sulfamoyl-benzo(f)quinoxaline) also blocked the response to 100 mM glutamate with pIC50 - again in agreement with published data. Functional channel expression (fluorescence signal) over time was monitored using the FLIPR system. Channel expression is robust over 28 passages.

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.

Glutamate receptors are the predominant excitatory neurotransmitter receptors in the mammalian brain and are activated in a variety of normal neurophysiologic processes. This gene product belongs to the kainate family of glutamate receptors, which are composed of four subunits and function as ligand-activated ion channels. The subunit encoded by this gene is subject to RNA editing at multiple sites within the first and second transmembrane domains, which is thought to alter the structure and function of the receptor complex. Alternatively spliced transcript variants encoding different isoforms have also been described for this gene. Mutations in this gene have been associated with autosomal recessive mental retardation.

FUNCTION: SwissProt: Q13002 # Ionotropic glutamate receptor. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L- glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist. May be involved in the transmission of light information from the retina to the hypothalamus.
SIZE: 908 amino acids; 102583 Da
SUBUNIT: Homotetramer or heterotetramer of pore-forming glutamate receptor subunits. Tetramers may be formed by the dimerization of dimers (Probable). Assembles into a kainate-gated homomeric channel that does not bind AMPA. GRIK2 associated to GRIK5 forms functional channels that can be gated by AMPA (By similarity). Interacts with DLG4.
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
TISSUE SPECIFICITY: Expression is higher in cerebellum than in cerebral cortex.
SIMILARITY: SwissProt: Q13002 ## Belongs to the glutamate-gated ion channel (TC 1.A.10) family.
MISCELLANEOUS: The postsynaptic actions of Glu are mediated by a variety of receptors that are named according to their selective agonists. This receptor binds domoate > kainate > quisqualate > 6- cyano-7-nitroquinoxaline-2,3-dione > L-glutamate = 6,7- dinitroquinoxaline-2,3-dione > dihydrokainate.

Human

Mycoplasma Testing:
The cell line has been screened to confirm the absence of Mycoplasma species

HEK

Ion Channel Cell Lines

Pack contains 2 vials of mycoplasma-free cells, 1 ml per vial

Upstate

293 cell line

2 x 1 ml aliquots

hGluR6

Q13002

Other Ligand Gated

2 x 1 ml aliquots

• GRIK2
• bA487F5.1
• MRT6
• MGC74427
• GLUR6
• GluR-6
• GLUK6
• GluR6
• GLR6
• EAA4

Ion Channels

PrecisION hGluR6-HEK Recombinant Cell Line

• NM_021956.2
• NM_175768.1

• GRIK2
• bA487F5.1
• MRT6
• MGC74427
• GLUR6
• GluR-6
• GLUK6
• GluR6
• GLR6
• EAA4