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
Protein Name:
CB1
Uniprot Number:
P21554
Protein Aliases:
CB1|CANN6
Gene Name:
CNR1
Gene ID:
1268
Gene Aliases:
CB1K5|CB-R|CB1|CANN6|CB1A
Accession Number:
XM_017010238
Organism:
Human
Construct Details:
Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist
Detection Method:
HTRF
Testing Information
Incubation:
30 min at 37°C
Control Activator:
CP55940
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 finµL 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:
16
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Adverse / Beneficial Action:
Cannabinoid CB1 receptor agonism, through modulation of neurotransmitter release, may attenuate nausea and vomiting in cancer chemotherapy, hyperalgesia and increased intestinal motility, and increase appetite stimulation in wasting syndromes. Adverse effects of receptor agonism may include alterations in cognition and memory, dysphoria/euphoria and sedation. CB1 receptor antagonism may reduce rewarding value of food intake and drug addiction.
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
RELATED SOLUTIONS