CB1 Rat Cannabinoid GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Two subtypes of the G-protein coupled cannabinoid receptor, CB1 and CB2, have been identified. CB1 couples to a pertussis-toxin sensitive G-protein to regulate Ca2+ currents, to activate inward rectifying K+ channels, and to activate MAP Kinases. High densities of CB1 receptors within the caudate-putamen, hippocampus and neocortex, suggests involvement in motor control, learning, and memory and cognitive function. Outside the CNS, CB1 expression is found in the testes, endothelial cells and ileum longitudinal smooth muscle.
Family:
GPCR
Sub Family:
Cannabinoid
Class:
Class A
Organism:
Rat
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Ligand:
[³H] SR141716A
Ligand Kd (nM):
0.7
Ligand Concentration:
0.5 nM
Non Specific:
10 µM R(+)-WIN-55,212-2
Incubation:
60 min at 25°C
Control Inhibitor:
R(+)-WIN-55,212-2
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
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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