Calcium Flux Assay

HTS039RTA - Ready-to-Assay™ D­2L Dopamine Receptor Frozen Cells

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    Dopamine is a catecholamine neurotransmitter that functions in the CNS to control locomotor, cognitive, emotional and neurendocrine processes, and in the periphery to modulate cardiovascular, renal and gastrointestinal processes.  The biological activities of dopamine are mediated by a family of five GPCRs.  The D1 and D5 subtypes couple to Gs to increase intracellular cAMP, whereas the D2, D3 and D4 subtypes couple to Gi to reduce cAMP (Missale et al., 1998). The D2 dopamine receptors have been of particular clinical interest due to their regulation of prolactin secretion and their affinity for antipsychotic drugs.  The D2 receptor exists as two alternatively spliced isoforms differing in the insertion of a stretch of 29 amino acids in the third intracellular loop (D2S and D2L) (Giros et al., 1989; Grandy et al., 1989). Cloned human D2L-expressing cell line is made in the Chem-7 host, which supports high levels of recombinant D2L expression and contains optimized levels of a recombinant promiscuous G protein 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 D2L.

    Additional Resource: HTS039RTA082214_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: NM_000795
    Protein Targets: D2L
    Target Sub-family: Dopamine
    Host Cell: Chem-7, a CHO-K1 cell line expressing a proprietary exogenous Gα protein
    Exogenous Gene Expression: DRD2 cDNA (Accession Number: NM_000795; see CODING SEQUENCE below).
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Grandy DK et al. (1989) Cloning of the cDNA and gene for a human D2 dopamine receptor. Proc Natl Acad Sci U S A.. 86:9762-6.
    Reference 2: 2. Giros B et al. (1989) Alternative splicing directs the expression of two D2 dopamine receptor isoforms. Nature. 342:923-6.
    Reference 3: 3. Missale C et al. (1998) Dopamine receptors: from structure to function. Physiol. Rev. 78: 189-225.