Calcium Flux Assay

HTS129C - ChemiScreen™ D5 Dopamine Receptor Stable Cell Line

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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 hypertensive phenotype of mice with a targeted deletion of D5 indicates that D5 regulates central control of sympathetic vascular tone (Hollon et al., 2002).  In addition, D5 modulates locomotion and corticostriatal long-term depression (Centonze et al., 2003). Cloned human D5-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant D5 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, antagonists and modulators at D5.

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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, cAMP Accumulation
    Host Cell: Chem-1, an adherent rat hematopoietic cell line expressing endogenous Gα15 protein.
    Exogenous Gene Expression: DRD5 cDNA (Accession Number: NM_000798; see CODING SEQUENCE below) expressed from a proprietary expressed from a proprietary pHS plasmid.
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Centonze D et al. (2003) Distinct roles of D1 and D5 dopamine receptors in motor activity and striatal synaptic plasticity. J. Neurosci. 23: 8506-8512.
    Reference 2: 2. Hollon TR et al. (2002) Mice lacking D5 dopamine receptors have increased sympathetic tone and are hypertensive. J. Neurosci. 22: 10801-10810.
    Reference 3: 3. Missale C et al. (1998) Dopamine receptors: from structure to function. Physiol. Rev. 78: 189-225.