HTS019M - ChemiSCREEN™ CB1 Cannabinoid Receptor Membrane Preparation

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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.  Ligands for CB1 include exogenous agonists such as D9-THC, the main psychoactive component of the plant Cannabis sativa, and endogenous eicosanoid agonists such as anandamide.  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. The CB1 membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression; thus, they are ideal HTS tools for screening for agonists and antagonists at CB1.  The membrane preparations exhibit a Kd of 7 nM for [3H]-SR141716A.  In the presence of 2 nM [3H]-SR141716A with CP55940 as unlabeled competitor, 10 mg/well CB1 Membrane Prep yields 4-fold signal-to-background ratio.

    Additional Resource :  HTS019M082514 Datasheet

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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, GTPγS Binding
    Species: Human CB1 (Accession number X54937)
    Host Cell: Chem-1, an adherent mammalian cell line without detectable endogenous CB1 expression.
    Reference 1: 1. Howlett AC et al. (2002) International Union of Pharmacology. XXVII. Classification of cannabinoid receptors. Pharmacol. Rev. 54: 161-202.