HTS033M - ChemiSCREEN™ GPR14 Urotensin II Receptor Membrane Preparation

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    Urotensin II, a cyclic 11-13 residue peptide expressed in motoneurons of the spinal cord, acts as a potent vasoconstrictor (Coulouarn et al., 1998; Ames et al., 1999). The effects of urotensin II are mediated by binding to a GPCR, GPR14, which is expressed in endothelium, smooth muscle, heart and pancreas (Ames et al., 1999). Genetic deletion of GPR14 in mice renders aortae refractile to the contractile activity of urotensin II without changing baseline hemodynamics (Behm et al., 2003). Pharmacological inhibition of urotensin II/GPR14 interactions prevents renal insufficiency following renal artery ligation (Clozel et al., 2004). Thus, GPR14 is an attractive target for a number of cardiovascular diseases. GPR14 Membrane Preparations are ideal tools for screening for antagonists of urotensin II/GPR14 interactions

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    Item Unit of Measure: EA
    Quantity: 200 units
    Storage: On receipt of material store at -70°C. Unopened reagent is stable for a minimum of 1 year from date of shipment when stored at recommended storage temperature. Avoid repeat freeze/thaw cycles. For maximum recovery of product, centrifuge original vial
    Applications: Radioligand Binding Assay
    Host Cell: Chem-2, a suspension mammalian cell line with no endogenous GPR14 expression.
    Reference 1: 1. Ames R.S., et al. (1999) Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14. Nature 401:282-286.
    Reference 2: 2. Behm D.J., et al. (2003) Deletion of the UT receptor gene results in the selective loss of urotensin-II contractile activity in aortae isolated from UT receptor knockout mice. Br. J. Pharmacol. 139: 464-72.
    Reference 3: 3. Clozel M., et al. (2004) Pharmacology of the urotensin-II receptor antagonist palosuran (ACT- 058362- 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role o
    Reference 4: 4. Coulouarn Y, et al. (1998) Cloning of the cDNA encoding the urotensin II precursor in frog and human reveals intense expression of the urotensin II gene in motoneurons of the spinal cord. Proc. Natl. Acad. Sci. USA 95: 15803-8.