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HTS020M - ChemiSCREEN™ CB2 Cannabinoid Receptor Membrane Preparation

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HTS020M
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    Cannabinoid compounds include exogenous drugs such as D9-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). CB2 membrane preparations are crude membrane preparations made from stable recombinant cell lines with a high-level of GPCR surface expression; thus, they are ideal HTS tools for screening for agonists and antagonists of CB2.

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    Item Unit of Measure: EA
    Quantity: 200 units
    Storage: On receipt of material store at -70°C. Unopened reagent is stable for a minimum of 1 year from date of shipment when stored at recommended storage temperature. Avoid repeat freeze/thaw cycles. For maximum recovery of product, centrifuge original vial
    Applications: Radioligand Binding Assay
    Species: Human CB2 (Accession number X74328)
    Host Cell: CHO.
    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.
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