Glutamate (NMDA, Non-Selective) Rat Ion Channel [3H] MK-801 Binding LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
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 coupled via GTP-binding proteins. The ligand-gated ion channels contain an integral cation channel that gate Na+ and in some cases Ca2+. MK-801 binding to the Glutamate NMDA receptor may cause Onley’s lesion, cognitive disruption and psychotic-spectrum reaction.
Family:
Ion Channel
Sub Family:
Glutamate (Ionotropic)
Class:
Ligand-Gated
Organism:
Rat
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Brains (except cerebella) membranes of Wistar derived rats weighing 175 ± 25 g are used to prepare glutamate NMDA receptors in Tris-HCl buffer pH 7.4. A 0.2 mg‡ aliquot is incubated with 5 nM [³H]MK-801 for 180 minutes at 25℃. Non-specific binding is estimated in the presence of 10 μM MK-801. Membranes are filtered and washed, the filters are then counted to determine [³H]MK-801 specifically bound. Compounds are screened at 10 μM.
Note: ‡Membrane protein may change from lot to lot, the concentration used will be adjusted if necessary.
Ligand:
[³H] MK-801
Ligand Kd (nM):
12
Ligand Concentration:
5 nM
Non Specific:
10 µM Dizocilpine ((+)-MK-801)
Incubation:
180 min at 25°C
Control Inhibitor:
Dizocilpine ((+)-MK-801)
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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