GABAA (Non-Selective) Rat Ion Channel [3H] Flunitrazepam Binding Agonist Radioligand LeadHunter Assay - FR
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
GABA is the major inhibitory transmitter in the mammalian central nervous system. GABAA receptors are anion channels gated by g-aminobutyric acid (GABA). Their amino acid sequences lie in the same superfamily as the nicotinic acetylcholine, glycine, serotonin 5-HT3 and ionic glutamate receptors, within the general class of ligand-gated ion channels. The majority of GABAA receptors carry some form of the Central Benzodiazepine subtype. GABAA Central Benzodiazepine receptor agonism has been shown to be anxiolytic, anticonvulsant, sedative, and may also impair motor function.
Family:
Ion Channel
Sub Family:
GABAA
Class:
Ligand-Gated
Protein Name:
GABAA (BZD site)
Uniprot Number:
P14867/P47870/P18507(human)
Gene Name:
GABRA1/GABRB2/GABRG2
Gene ID:
2554/2561/2566
Organism:
Rat
Tissue:
Brain
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[3H]flunitrazepam
Ligand Kd (nM):
2.1
Ligand Concentration:
0.4 nM
Non Specific:
3 µM Diazepam
Incubation:
60 min at 4°C
Control Inhibitor:
HYDROGEN DIAZEPAM CHLORIDE
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:
10 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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