HTS039C2 - ChemiSCREEN™ D2L 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 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). Eurofins' cloned human D2L-expressing cell line is made in the CHO host, which supports optimal levels of recombinant D2L expression for robust agonist-induced cAMP signal. Thus, the cell line is an ideal tool for screening for agonists and antagonists at the D2L Receptor.

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    Item Unit of Measure: PK
    Contents: 2 vials of mycoplasma-free cells, 1 ml per vial.
    Storage: Vials are to be stored in liquid N2.
    Applications: cAMP Accumulation
    Entrez Gene Number: NM_000795
    Host Cell: Chem-1, an adherent rat hematopoietic cell line expressing endogenous Gα15 protein
    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. USA 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.
    Reference 4: 4. Moreland RB et al. (2004) Comparative pharmacology of human dopamine D2-like receptor stable cell lines coupled to calcium flux through Gαqo5. Biochem. Pharmacol. 68:761-772.