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HTS020RTA - Ready-to-Assay™ CB2 Cannabinoid Receptor Frozen Cells

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    CB1 is a GPCR that is expressed primarily in brain and nervous tissue, and mediates numerous CNS responses such as analgesia, appetite, cognition, memory and locomotor activity.  A number of cannabinoid ligands bind to CB1 and activate Gi/o-mediated downstream responses, including inhibition of cAMP production and activation of ion channels and MAP kinases.  Such ligands include exogenous agonists such as Δ9-THC, the main psychoactive component of the plant Cannabis sativa, and endogenous agonists such as anandamide that belong to eicosanoid family.  A number of synthetic agonists such as CP55940 and R-(+)-WIN55212, and antagonists, such as SR141716A, for CB1 have been developed (Howlett et al., 2002).  CB1 agonists have clinical utility in analgesia and antiemetic properties, whereas CB1 antagonists show promise for treatment of appetite in obesity disorders. Cloned human CB1-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant CB1 expression on the cell surface and contains high levels of the promiscuous G protein Gα15 to couple the receptor to the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for agonists, antagonists and modulators at CB1.

    Additional Resource: HTS020RTA092414_Datasheet

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    Item Unit of Measure: PK
    Contents: Pack contains 2 vials of mycoplasma-free cells, 1 ml per vial. Fifty (50) mL of Media Component.
    Storage: Vials are to be stored in liquid N2.
    Applications: Calcium Flux Assay
    Entrez Gene Number: X74328
    Protein Targets: CB2
    Target Sub-family: Cannabinoid
    Host Cell: Chem-4, an adherent rat hematopoietic cell line expressing endogenous G15 protein as well as an exogenous proprietary promiscuous Gα protein
    Exogenous Gene Expression: CNR2 cDNA (Accession Number: X74328) expressed from a proprietary plasmid.
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Howlett AC et al. (2002) International Union of Pharmacology. XXVII. Classification of cannabinoid receptors. Pharmacol. Rev. 54: 161-202.
    Reference 2: 2. Ibrahim MM et al. (2005) CB2 cannabinoid receptor activation produces antinociception by stimulating peripheral release of endogenous opioids. Proc. Natl. Acad. Sci. USA 102: 3093-8.
    Reference 3: 3. Julien B et al. (2005) Antifibrogenic role of the cannabinoid receptor CB2 in the liver. Gastroenterology 128: 742-755.
    Reference 4: 4. Ofek O et al. (2006) Peripheral cannabinoid receptor, CB2, regulates bone mass. Proc. Natl. Acad. Sci. USA 103: 696-701.