Calcium Flux Assay

HTS046C - ChemiSCREEN™ Human Recombinant ETB Endothelin Receptor Calcium-Optimized Stable Cell Line

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    The endothelin family of peptides are potent vasoconstrictors synthesized by endothelial cells in both constitutive and inducible pathways.  The biological actions of endothelins are mediated by two GPCRs, ETA and ETB (Davenport, 2002).   Whereas ETA is the predominant receptor on smooth muscle cells and thus is the primary mediator of the vasoconstrictor activity, ETB is found on endothelial cells and mediates vasodilation (Nilsson et al., 1997).  In addition, ETB has also been linked to renal failure, congestive heart failure, atherosclerosis, and pulmonary hypertension (D’Orléans-Juste, et al., 2002).  A mutation in ETB has been found to cause Hirschsprung disease-2, a degenerative disease of the digestive tract (Puffenberger et al, 1994). Cloned human ETB receptor-expressing ChemiScreen cells were constructed by stable transfection of CHO cells with ETB.  These stability-tested cells are ready for fluorescence-based assays for agonists, antagonists and modulators at the ETB receptor. 

    Additional Resource :  HTS046C112014 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-8
    Exongenous Gene Expression: EDNRB cDNA (Accession Number: NM_000115- see CODING SEQUENCE below) expressed from a proprietary pHS plasmid.
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Davenport AP (2002) International Union of Pharmacology. XXIX. Update on Endothelin Receptor Nomenclature. Pharmacol. Rev. 54: 219-226.
    Reference 2: 2. Nilsson T, et al. (1997) Presence of contractile endothelin-A and dilatory endothelin-B receptors in human cerebral arteries. Neurosurgery. 40: 346–351-comment 351–353
    Reference 3: 3. D’Orléans-Juste P, et al (2002) Function of the endothelinB receptor in cardiovascular physiology and pathophysiology. Pharmacol Ther. 95: 221-238.
    Reference 4: 4. Puffenberger EG, et al (1994) A missense mutation of the endothelin-B receptor gene in multigenic Hirschsprung's disease. Cell 79: 1257-1266.