CB1 Human Cannabinoid GPCR GTPgammaS Agonist LeadHunter Assay - TW

Item: 306000-0

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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

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:

Full Length, Recombinant

Cell Type:

Chem-1

Assay Information

Assay Type:

Functional

Assay Sub Type:

GTPgammaS

Functional Mode:

Agonist

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Human recombinant cannabinoid CB1 receptors stably expressed in Chem-1 cells are used. Test compound and/or vehicle is preincubated with the membranes (0.045 mg/ml‡) and 10 µM GDP in modified HEPES pH 7.4 buffer for 20 minutes and SPA beads are then added for another 60 minutes at 30°C. The reaction is initiated by 0.3 nM [35S]GTPgS for an additional 30 minute incubation period. Test compound-induced increase of [35S]GTPgS binding by 50 percent or more (≥50%) relative to the 1 μM CP 55,940 response indicates possible cannabinoid CB1 receptor agonist activity. Note: ‡Membrane protein may change from lot to lot, the concentration used will be adjusted if necessary.

Incubation:

30 min at 30°C

Control Activator:

CP55940

Criteria For Significance:

≥ 50% Increase in bound [35S]GTPgammaS relative to CP55,940 response, ≥ 50% Inhibition of CP55,940-induced bound [35S]GTPgammaS

Test Concentration / Dose:

Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM

Test Sample Requirements:

75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)

Minimum Order Quantity:

Turnaround Time

Standard:

20 Business Days

Reference Compound Data

PubChem ID

104895

Name

CP55940

Measurement

0.002μM - EC50

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:

Taiwan - Taipei