Calcium Flux Assay

HTS020C - ChemiScreen™ Human Recombinant CB2 Cannabinoid Receptor Calcium-Optimized Stable Cell Line

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    Cannabinoid compounds include exogenous drugs such as 9-THC, the main psychoactive component of the plant Cannabis sativa, and endogenous mediators, such as anandamide, that belong to eicosanoid family.The biological effects of cannabinoids are mediated by a family of two Gi-coupled 7-transmembrane receptors, CB1 and CB2.  The CB1 receptor is found primarily in brain and mediates the psychoactive effects of cannabinoid ligands.  The CB2 receptor is expressed mainly in immune cells, including mast cells and CD40-activated B cells, where it mediates proliferation and inhibition of migration (Howlett et al., 2002).  Activation of CB2 inhibits the development of liver fibrosis (Julien et al., 2005).  In bone, CB2 is expressed in both osteoblasts and osteoclasts, and functions to prevent bone loss (Ofek et al., 2006).  In addition, activation of CB2 has an antinociceptive effect in animal models of neuropathic, inflammatory, and acute pain; this effect is mediated by release of endogenous opioids in the periphery (Ibrahim et al., 2005).  The cloned human CB2 –expressing cell line is made in the Chem-4 host, which supports high levels of recombinant CB2 expression on the cell surface and contains high levels of promiscuous G proteins to couple the receptor to the calcium signaling pathway.  Thus, the cell line is an ideal tool for screening for antagonists of interactions between CB2 and its ligands.  

    Additional Resource :  HTS020C050515 Datasheet

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    Contents: 2 vials of mycoplasma-free cells, 1 ml per vial.
    Storage: Vials are to be stored in liquid N2.
    Applications: Calcium Flux Assay
    Host Cell: Chem-4, an adherent cell line expressing the promiscuous G-protein, Gα15.
    Exongenous Gene Expression: Human CB2 cDNA (Accession Number: X74328) and promiscuous G protein are expressed in a bicistronic vector
    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.Holst B. et al. (2007) GPR39 signaling is stimulated by zinc ions but not by obestatin. Endocrinology 148:
    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.