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:

Antagonist

Detection Method:

HTRF

Testing Information

Incubation:

30 min at 37°C

Control Inhibitor:

AM 281

Control Activator:

CP 55940 (1 nM)

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

PubChem ID

4302962

Name

AM 281

Measurement

39nM - IC50

PubChem ID

2125

Name

AM251

Measurement

6nM - IC50

PubChem ID

4302963

Name

AM630

Measurement

- IC50

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

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