Biological Information

Background Information:

Cannabinoid receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Cannabinoid CB1 receptors are found primarily in brain and nervous tissue. 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.

cAMP Hunter™ Gi cell lines overexpress naturally Gi coupled, wild type GPCRs and are designed to detect inhibition of intracellular cAMP production in response to agonist stimulation of the receptor. These cell lines are designed to be used in conjunction with the HitHunter® cAMP Assay Detection Kit.

Family:

GPCR

Sub Family:

Cannabinoid

Class:

Class A

Coupling:

Gi/Go

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:

AY225225

Organism:

Human

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Testing Information

Control Activator:

CP55940

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 10 concentrations are selected

Test Sample Requirements:

40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)

Minimum Order Quantity:

20

Turnaround Time

Standard:

15 Business Days

Clinical Relevance

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:

USA - Fremont, CA