HTS019C - ChemiSCREEN™ Human CB1 Cannabinoid Receptor Calcium-Optimized Stable Cell Line

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HTS019C
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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 D9-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.  The 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 and antagonists of CB1.

    Additional Resource :  HTS019C050515 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-1, an adherent cell line expressing the promiscuous G-protein, Gα15.
    Exongenous Gene Expression: Human CB1 cDNA (Accession Number: X54937) 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.
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